TXX-522 | CB1R antagonist | Probechem Biochemicals

Chemical Structure : TXX-522

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TXX-522 (TXX522)

货号: PC-28693Not For Human Use, Lab Use Only.

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100 mg		Get quote

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生物&药学活性

TXX-522 is a potent, selective and peripherally restricted cannabinoid 1 receptor (CB1R) antagonist/inverse agonist with Ki and IC50 of 0.15 uM and 0.17 uM respectively, >100-fold selecive over CB2 receptor.
binds with the CB1R in a mode similar to that of SR141716A.
TXX-522 shows good binding, CB1R-selectivity (over the CB2R), and functional antagonist activities in a range of in vitro molecular and cellular assays.
TXX-522 shows minimal brain penetration.
TXX-522 has good oral bioavailability and a potent anti-obesity effect, and ameliorates insulin resistance in high-fat diet-induced obese mice.

物理化学性质&存储条件

分子量	478.78
分子式	C20H14Cl3N5OS
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-(5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazol-3-yl)-3-(thiazol-2-yl)urea

参考文献

1. Chen W, et al. Front Pharmacol. 2017 Oct 5;8:707.

TXX-522 (TXX522)

生物&药学活性

物理化学性质&存储条件

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TXX-522 (TXX522)

生物&药学活性

物理化学性质&存储条件

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