CH 223191

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CH 223191

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

301326-22-7

包装与价格：

包装	价格(元)
10mg	电议
50mg	电议

产品介绍

化学性质

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	333.39
Cas No.	301326-22-7
Formula	C₁₉H₁₉N₅O
Solubility	≥33.3 mg/mL in DMSO; insoluble in H2O; ≥2.31 mg/mL in EtOH
Chemical Name	2-methyl-N-[2-methyl-4-[(2-methylphenyl)diazenyl]phenyl]pyrazole-3-carboxamide
Canonical SMILES	CC1=CC=CC=C1N=NC2=CC(=C(C=C2)NC(=O)C3=CC=NN3C)C
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

CH 223191 is a potent aryl hydrocarbon receptor (AhR) antagonist with an IC₅₀value of 30 nM [1].

The aryl hydrocarbon receptor (AhR) is a cytosolic ligand-activated basic helix-loop-helix transcription factor. The toxicities of 2, 3, 7, 8-Tetrachlorodibenzo-p-dioxin (TCDD) are mostly mediated by binding and activating AhR, which causes nuclear signal transduction and adverse effects.

CH 223191 inhibits TCDD-induced AhR-dependent transcriptioninvitro. By the HepG2-DER-luc-cell-based assay, CH 223191 showed the most potent inhibitory (IC₅₀=0.03±0.005 mΜ). CH 223191 had no agonist-like effect (at concentrations up to 100 μM) compared with known AhR antagonists such as resveratrol and α-naphthoflavone. Besides, CH 223191 had no effect on estrogen receptor-mediated luciferase activity while flavone potentiated that in MCF-7 breast cancer cells [1].

Male mice were administrated with vehicle or CH 223191 (10mg/kg) orally once a day for 25 days and treated with TCDD (100μg/kg) once after the first week of CH 223191 administration. Expression of cytochrome P450 1A1protein from extracts of the liver was quantitated, which showed significant suppression by treatment of CH 223191 (10 mg/kg). By measuring plasma AST and ALT levels, the level of TCDD-induced toxicity was decreased apparently by CH 223191. By measuring body weights, the drug significantly avoided the symptoms of severe wasting caused by TCDD [1].

Reference:

[1]. Kim S-H, Henry E C, Kim D-Y, et al. Novel Compound 2-Methyl-2H-pyrazole-3-carboxylic Acid (2-methyl-4-o-tolylazo-phenyl)-amide (CH-223191) Prevents 2,3,7,8-TCDD-Induced Toxicity by Antagonizing the Aryl Hydrocarbon Receptor. Molecular pharmacology, 2006, 69(6):1871-1878.