Month: January 2023

CYP450s-activity relations of celastrol to interact with triptolide reveal the reasons of hepatotoxicity of Tripterygium wilfordii was written by Jin, Chunhuan;Wu, Zijun;Wang, Lili;Kanai, Yoshikatsu;He, Xin. And the article was included in Molecules in 2019.Product Details of 1614-12-6 This article mentions the following:

Celastrol and triptolide, as the two main bio-activity ingredients in Tripterygium wilfordii, have wide anticancer pharmacol. potency, as well as anti-inflammatory and immunosuppression effects. However, they have potential hepatotoxicity and underlying mechanisms of them-induced toxicity mediated by hepatic CYP450s have not been well delineated. In the present study, we accessed the toxic effects and possible mechanism of celastrol and triptolide on primary rat hepatocytes. Models of subdued/enhanced activity of CYP450 enzymes in primary rat hepatocytes were also constructed to evaluate the relationship between the two ingredients and CYP450s. LC-MS/MS was used to establish a detection method of the amount of triptolide in rat hepatocytes. As the results, cell viability, biochem. index, and mitochondrial membrane potential indicated that celastrol and triptolide had toxic potencies on hepatocytes. Moreover, the toxic effects were enhanced when the compounds combined with 1-aminobenzotriazole (enzyme inhibitor) while they were mitigated when combined with phenobarbital (an enzyme inducer). Meanwhile, celastrol could affect the amount of triptolide in the cell. We therefore put forward that increase of triptolide in the cell might be one of the main causes of hepatotoxicity caused by Tripterygium wilfordii. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Product Details of 1614-12-6).

1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. The triazole ring is a relatively stable functional group, and the triazole bond can be used for a variety of applications, such as replacing the phosphate backbone of DNA. Due to the structural characteristics, both 1,2,3- and 1,2,4-triazoles are able to accommodate a broad range of substituents (electrophiles and nucleophiles) around the core structures and pave the way for the construction of diverse novel bioactive molecules.Product Details of 1614-12-6

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Preliminary evaluation of Pleurotus ostreatus for the removal of selected pharmaceuticals from hospital wastewater was written by Palli, Laura;Castellet-Rovira, Francesc;Perez-Trujillo, Miriam;Caniani, Donatella;Sarra-Adroguer, Montserrat;Gori, Riccardo. And the article was included in Biotechnology Progress in 2017.Recommanded Product: 1614-12-6 This article mentions the following:

The fungus Pleurotus ostreatus was investigated to assess its ability to remove diclofenac, ketoprofen, and atenolol spiked at 10 mg/L each one in hospital wastewater. The degradation test was carried out in a fluidized bed bioreactor testing both the batch and the continuous mode (hydraulic retention time in the range 1.63-3 days). In batch mode, diclofenac disappeared in less than 24 h, ketoprofen was degraded up to almost 50% in 5 days while atenolol was not removed. In continuous mode, diclofenac and ketoprofen removals were about 100% and 70% resp.; atenolol degradation was negligible during the first 20 days but it increased up to 60% after a peak of laccase production and notable biomass growth. In order to identify the enzymic system involved, further experiments were carried out in flasks. Purified laccase completely transformed atenolol and diclofenac in less than 5 h, but not ketoprofen. In vivo experiments suggested that cytochrome P 450 could be involved in diclofenac and ketoprofen degradation, while partial correlation studies confirmed the role of laccase in atenolol and diclofenac degradation Two intermediates of diclofenac and ketoprofen were detected by NMR. Moreover P. ostreatus was able to reduce COD of the hospital wastewater which is an important advantage comparing to other fungi in order to develop a wastewater treatment process. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Recommanded Product: 1614-12-6).

1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. The triazole ring is a relatively stable functional group, and the triazole bond can be used for a variety of applications, such as replacing the phosphate backbone of DNA. Many triazoles have antifungal effects: the triazole antifungal drugs include fluconazole, isavuconazole, itraconazole, voriconazole, pramiconazole, ravuconazole, and posaconazole and triazole plant-protection fungicides include epoxiconazole, triadimenol, myclobutanil, propiconazole, prothioconazole, metconazole, cyproconazole, tebuconazole, flusilazole and paclobutrazol.Recommanded Product: 1614-12-6

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Highly N²-Selective Palladium-Catalyzed Arylation of 1,2,3-Triazoles was written by Ueda, Satoshi;Su, Ming-Juan;Buchwald, Stephen L.. And the article was included in Angewandte Chemie, International Edition in 2011.Application In Synthesis of 4-(2H-1,2,3-Triazol-2-yl)benzaldehyde This article mentions the following:

Exceptional levels of N² selectivity can be obtained in the palladium-catalyzed N-arylation of simple 1,2,3-triazoles by the use of the very bulky biarylphosphine ligand I. This method enabled the first highly N²-selective arylation of 4-substituted and 4,5-unsubstituted 1,2,3-triazoles with aryl bromides, chlorides, and triflates. E.g., in presence of Pd₂(dba)₃, ligand I, and K₃PO₄, arylation of 3-(1,2,3-triazol-4-yl)pyridine (prepared from TMSN₃ and 3-ethynylpyridine) with 3,5-dimethoxybromobenzene gave 86% 3-[2-(3,5-dimethoxyphenyl)-2H-1,2,3-triazol-4-yl]pyridine (II). In the experiment, the researchers used many compounds, for example, 4-(2H-1,2,3-Triazol-2-yl)benzaldehyde (cas: 179056-04-3Application In Synthesis of 4-(2H-1,2,3-Triazol-2-yl)benzaldehyde).

4-(2H-1,2,3-Triazol-2-yl)benzaldehyde (cas: 179056-04-3) belongs to triazole derivatives. The many free lone pairs in triazoles make them useful as coordination compounds, although not typically as haptic ligands. Triazole growth retardants such as uniconazole and paclobutrazol have been known to inhibit the biosynthesis of gibberellins by blocking kaurene oxidase, an P450 enzymeApplication In Synthesis of 4-(2H-1,2,3-Triazol-2-yl)benzaldehyde

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Three-dimensional (3D) HepaRG spheroid model with physiologically relevant xenobiotic metabolism competence and hepatocyte functionality for liver toxicity screening was written by Ramaiahgari, Sreenivasa C.;Waidyanatha, Suramya;Dixon, Darlene;De Vito, Michael J.;Paules, Richard S.;Ferguson, Stephen S.. And the article was included in Toxicological Sciences in 2017.Category: triazoles This article mentions the following:

Effective prediction of human responses to chem. and drug exposure is of critical importance in environmental toxicol. research and drug development. While significant progress has been made to address this challenge using in vitro liver models, these approaches often fail due to inadequate tissue model functionality. Herein, the authors describe the development, optimization, and characterization of a novel three-dimensional (3D) spheroid model using differentiated HepaRG cells that achieve and maintain physiol. relevant levels of xenobiotic metabolism (CYP1A2, CYP2B6, and CYP3A4/5). This in vitro model maintains a stable phenotype over multiple weeks in both 96- and 384-well formats, supports highly reproducible tissue-like architectures and models pharmacol.- and environmentally important hepatic receptor pathways (ie AhR, CAR, and PXR) analogous to primary human hepatocyte cultures. HepaRG spheroid cultures use 50-100× fewer cells than conventional two dimensional cultures, and enable the identification of metabolically activated toxicants. Spheroid size, time in culture and culture media composition were important factors affecting basal levels of xenobiotic metabolism and liver enzyme inducibility with activators of hepatic receptors AhR, CAR and PXR. Repeated exposure studies showed higher sensitivity than traditional 2D cultures in identifying compounds that cause liver injury and metabolism-dependent toxicity. This platform combines the well-documented impact of 3D culture configuration for improved tissue functionality and longevity with the requisite throughput and repeatability needed for year-over-year toxicol. screening. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Category: triazoles).

1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. Many triazoles are versatile, biologically active compounds commonly used as fungicides and plant retardants. 1,2,3-Triazoles are usually prepared following (3+2) cycloaddition protocols. A common technique for unsubstituted triazoles is the Huisgen azide-alkyne 1,3-dipolar cycloaddition: a azide and an alkyne react at high temperature to form a ring. However, the Huisgen strategy produces a mixture of isomers (typically 1,4- and 1,5-disubstituted) when used to produce substituted triazoles.Category: triazoles

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Human CYP enzyme-activated genotoxicity of 2,2,4,4-tetrabromobiphenyl ether in mammalian cells was written by Song, Meiqi;Wang, Yujian;Chen, Zhihong;Gao, Hongbin;Yang, Zongying;Yu, Hang;Liu, Yungang. And the article was included in Chemosphere in 2022.HPLC of Formula: 1614-12-6 This article mentions the following:

Polybrominated biphenyl ethers (PBDEs) are a group of persistent organic pollutants with endocrine-disrupting, neurotoxic, tumorigenic and DNA-damaging activities. They are hydroxylated by human liver microsomal CYP enzymes, however, their mutagenicity remains unknown. In this study, 2,2,4,4-tetrabromobiphenyl ether (BDE-47, relatively abundant in human tissues) was investigated for micronuclei induction and DNA damage in mammalian cells. The results indicated that BDE-47 up to 80 μM under a 6 h/18 h (exposure/recovery, covering 2 cell cycles) regime did not induce micronuclei in V79-Mz and V79-derived cell lines expressing human CYP1A1 or 1A2, while it was moderately pos. in human CYP2B6-, 2E1-and 3A4-expressing cell lines (V79-hCYP2B6, V79-hCYP2E1-hSULT1A1 and V79-hCYP3A4-hOR, resp.). Following 24 h exposure, BDE-47 induced micronuclei in V79-hCYP2E1-hSULT1A1 and V79-hCYP3A4 cells at increased potencies. In the human hepatoma (HepG2) cells BDE-47 (48 h exposure) was inactive up to 40 μM, however, pretreatment of the cells with ethanol (0.2%, v:v, inducer of CYP2E1) or rifampicin (10 μM, inducer of CYP3A4) led to significant micronuclei formation by BDE-47; pretreatment with bisphenol AF (100 nM) also potentiated BDE-47-induced micronuclei formation (which was blocked by a CYP2E1 inhibitor trans-1,2-dichloroethylene or a CYP3A inhibitor (ketoconazole). Immunofluorescent staining of centromere protein B with the micronuclei formed by BDE-47 in HepG2 cells pretreated with ethanol or rifampicin demonstrated selective formation of centromere-containing micronuclei. The increased phosphorylation of both histones H2AX and H3 in HepG2 by BDE-47 also indicated an aneugenic potential. Therefore, this study suggests that BDE-47 is an aneugen activated by several human CYP enzymes. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6HPLC of Formula: 1614-12-6).

1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. Triazoles consist of a five-membered ring containing three nitrogen atoms and are biologically active, especially as antifungal, antimicrobial and enzyme inhibitors.Triazole heterocyclic structures are found to form many weak nonbond interactions with the receptors and enzymes in biological systems.HPLC of Formula: 1614-12-6

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu₄) was written by Gogliotti, Rocco D.;Blobaum, Anna L.;Morrison, Ryan M.;Daniels, J. Scott;Salovich, James M.;Cheung, Yiu-Yin;Rodriguez, Alice L.;Loch, Matthew T.;Conn, P. Jeffrey;Lindsley, Craig W.;Niswender, Colleen M.;Hopkins, Corey R.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2016.Computed Properties of C6H6N4 This article mentions the following:

Herein the authors report the synthesis and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as novel pos. allosteric modulators of mGlu₄. The authors detail the authors’ work towards finding Ph replacements for the core scaffold of previously reported Ph sulfonamides and Ph sulfone compounds The authors’ efforts culminated in the identification of N-(1-((3,4-dimethylphenyl)sulfonyl)-1H-pyrrol-3-yl)picolinamide as a potent PAM of mGlu₄. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Computed Properties of C6H6N4).

1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. Triazoles exhibit substantial isomerism, depending on the positioning of the nitrogen atoms within the ring. Both the triazoles and their derivatives have significant biological properties including antimicrobial, antiviral, antitubercular, anticancer, anticonvulsant, analgesic, antioxidant, anti-inflammatory, and antidepressant activities.Computed Properties of C6H6N4

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Characterization of T-cell responses to SMX and SMX-NO in co-trimoxazole hypersensitivity patients expressing HLA-B*13:01 was written by Pratoomwun, Jirawat;Thomson, Paul;Jaruthamsophon, Kanoot;Tiyasirichokchai, Rawiporn;Jinda, Pimonpan;Rerkpattanapipat, Ticha;Tassaneeyakul, Wichittra;Nakkam, Nontaya;Rerknimitr, Pawinee;Klaewsongkram, Jettanong;Srinoulprasert, Yuttana;Pirmohamed, Munir;Naisbitt, Dean J.;Sukasem, Chonlaphat. And the article was included in Frontiers in Immunology in 2021.Application In Synthesis of 1H-Benzo[d][1,2,3]triazol-1-amine This article mentions the following:

HLA-B*13:01-pos. patients in Thailand can develop frequent co-trimoxazole hypersensitivity reactions. This study aimed to characterize drug-specific T cells from three co-trimoxazole hypersensitive patients presenting with either Stevens-Johnson syndrome or drug reaction with eosinophilia and systemic symptoms. Two of the patients carried the HLA allele of interest, namely HLA-B*13:01. Sulfamethoxazole and nitroso sulfamethoxazole specific T cell clones were generated from T cell lines of cotrimoxazole hypersensitive HLA-B*13:01-pos. patients. Clones were characterized for antigen specificity and cross-reactivity with structurally related compounds by measuring proliferation and cytokine release. Surface marker expression was characterized via flow cytometry. Mechanistic studies were conducted to assess pathways of T cell activation in response to antigen stimulation. Peripheral blood mononuclear cells from all patients were stimulated to proliferate and secrete IFN-g with nitroso sulfamethoxazole. All sulfamethoxazole and nitroso sulfamethoxazole specific T cell clones expressed the CD4+ phenotype and strongly secreted IL-13 as well as IFN-g, granzyme B and IL-22. No secretion of IL-17 was observed A number of nitroso sulfamethoxazole-specific clones cross-reacted with nitroso dapsone but not sulfamethoxazole whereas sulfamethoxazole specific clones cross-reacted with nitroso sulfamethoxazole only. The nitroso sulfamethoxazole specific clones were activated in both antigen processingdependent and -independent manner, while sulfamethoxazole activated T cell responses via direct HLA binding. Furthermore, activation of nitroso sulfamethoxazole-specific, but not sulfamethoxazole-specific, clones was blocked with glutathione. Sulfamethoxazole and nitroso sulfamethoxazole specific T cell clones from hypersensitive patients were CD4+ which suggests that HLA-B*13:01 is not directly involved in the iatrogenic disease observed in co-trimoxazole hypersensitivity patients. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Application In Synthesis of 1H-Benzo[d][1,2,3]triazol-1-amine).

1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. Many triazoles are versatile, biologically active compounds commonly used as fungicides and plant retardants. Both the triazoles and their derivatives have significant biological properties including antimicrobial, antiviral, antitubercular, anticancer, anticonvulsant, analgesic, antioxidant, anti-inflammatory, and antidepressant activities.Application In Synthesis of 1H-Benzo[d][1,2,3]triazol-1-amine

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Two cobalt complexes derived from 1H-1,2,3-triazole-4,5-dicarboxylic acid: Syntheses, structures and magnetic properties was written by Li, Ling;Zou, Ji-Yong;Gu, Zhen;You, Sheng-Yong;Chen, Yan-Hua;Xia, Jun;Cui, Jian-Zhong. And the article was included in Inorganic Chemistry Communications in 2016.Formula: C4H3N3O4 This article mentions the following:

Two cobalt(II) homometallic complexes, [Co₂(HTDA)₂(H₂O)₆·2H₂O] (1) and {[Co₃(TDA)₂(H₂O)₈]·H₂O}_n (2) (H₃TDA = 1H-1,2,3-triazole-4,5-dicarboxylic acid) were synthesized and structurally characterized. Single-crystal x-ray crystallog. study reveals that they crystallize in trigonal space group orthorhombic Pna2₁, resp. In 1, two Co^2 + cations are bonded by two HTDA^2 – ligands to generate a binuclear Co^II unit, which can further be extended to a 3-dimensional supermol. structure via the hydrogen bonds. At variance with 1, the nearest Co^2 + cations of 2 are connected via TDA^3 – ligands to form a 1-dimensional coordination polymer and can be further linked to each other to result in a 3-dimensional supermol. framework through the hydrogen bonding interactions as well. The magnetic properties of them were studied. In the experiment, the researchers used many compounds, for example, 1H-1,2,3-Triazole-4,5-dicarboxylic acid (cas: 4546-95-6Formula: C4H3N3O4).

1H-1,2,3-Triazole-4,5-dicarboxylic acid (cas: 4546-95-6) belongs to triazole derivatives. Among the nitrogen-containing heterocyclic compounds, triazoles emerge with superior pharmacological applications.Triazole heterocyclic structures are found to form many weak nonbond interactions with the receptors and enzymes in biological systems.Formula: C4H3N3O4

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Zinc (II) Chloride as Phase Transfer Catalyst and as Catalyst of Cycloaddition Azide Ion to Heterocumulenes and Terminal Alkynes in Organic Solvents was written by Vorona, Svetlana V.;Zevatskii, Yuri E.;Myznikov, Leonid V.. And the article was included in ChemistrySelect in 2019.Related Products of 40594-98-7 This article mentions the following:

The system of NaN₃-ZnCl₂ in organic solvents was effective for azide ion cycloaddition to heterocumulenes and terminal alkynes. The reaction proceeded readily in the case of heterocumulenes, so these transformations fall into the category of click reactions. The study on the reaction mechanism showed that role of zinc salt consists in transferring azide ion to the organic phase and decreasing the energy barrier of nucleophilic addition of azide ion to the unsaturated substrate. In the experiment, the researchers used many compounds, for example, Ethyl 1H-1,2,3-triazole-5-carboxylate (cas: 40594-98-7Related Products of 40594-98-7).

Ethyl 1H-1,2,3-triazole-5-carboxylate (cas: 40594-98-7) belongs to triazole derivatives. Many triazoles are versatile, biologically active compounds commonly used as fungicides and plant retardants. Triazole growth retardants such as uniconazole and paclobutrazol have been known to inhibit the biosynthesis of gibberellins by blocking kaurene oxidase, an P450 enzymeRelated Products of 40594-98-7

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Resistance to dicyclanil and imidacloprid in the sheep blowfly, Lucilia cuprina, in Australia was written by Kotze, Andrew C.;Bagnall, Neil H.;Ruffell, Angela P.;George, Sarah D.;Rolls, Nicholas M.. And the article was included in Pest Management Science in 2022.Recommanded Product: 1614-12-6 This article mentions the following:

The sheep blowfly, Lucila cuprina, is a myiasis-causing parasite responsible for significant production losses and welfare issues for the Australian sheep industry. Control relies largely on the use of insecticides. The pyrimidine compound, dicyclanil, is the predominant control chem., although other insecticides also are used, including imidacloprid, ivermectin, cyromazine and spinosad. We investigated in vitro resistance patterns and mechanisms in field-collected blowfly strains. The Walgett 2019 strain showed significant levels of resistance to both dicyclanil and imidacloprid, with resistance factors at the IC50 of 26- and 17-fold, resp., in in vitro bioassays. Co-treatment with the cytochrome P 450 inhibitor, aminobenzotriazole, resulted in significant levels of synergism for dicyclanil and imidacloprid (synergism ratios of 7.2- and 6.1-fold, resp.), implicating cytochrome P 450 in resistance to both insecticides. Cyp12d1 transcription levels were increased up to 40-fold throughout the larval life stages in the resistant strain compared to a reference susceptible strain, whereas transcription levels of some other cyp genes (6g1, 4d1, 28d1) did not differ between the strains. Similar resistance levels also were observed in flies collected from the same property in two subsequent years. This study indicates that in vitro resistance to both dicyclanil and imidacloprid in this field-collected blowfly strain is likely mediated by cytochrome P 450, with Cyp12d1 implicated as the enzyme responsible; however, it remains possible that another P 450 also may be involved. A common resistance mechanism for the two drugs has important implications for drug rotation strategies designed to prolong the useful life of flystrike control chems. 2022 The Authors. Pest Management Science published by John Wiley & Sons Ltd on behalf of Society of Chem. Industry. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Recommanded Product: 1614-12-6).

1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. Triazoles exhibit substantial isomerism, depending on the positioning of the nitrogen atoms within the ring. Triazoles are compounds with a vast spectrum of applications, varying from materials (polymers), agricultural chemicals, pharmaceuticals, photoactive chemicals and dyes.Recommanded Product: 1614-12-6

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics