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首页-小分子抑制剂&激动剂-GPCR-Cannabinoid Receptor-Taranabant
Taranabant

Chemical Structure : Taranabant

CAS No.: 701977-09-5

Taranabant (MK-0364;MK0364)

货号: PC-42063Not For Human Use, Lab Use Only.

Taranabant (MK-0364) is a potent, selective and orally active cannabinoid-1 receptor (CB1R) inverse agonist with IC50 of 2.8 nM, Ki of 0.13 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Taranabant (MK-0364) is a potent, selective and orally active cannabinoid-1 receptor (CB1R) inverse agonist with IC50 of 2.8 nM, Ki of 0.13 nM.
Taranabant displays >1000-fold selectivity over CB2R (Ki=170 nM), AT1R, NK2R, A3R, MT1R, D1R, etc.
Taranabant dose-dependently inhibits food intake and weight gain in diet-induced obese (DIO) rats with an acute minimum effective dose of 1 mg/kg and has good pharmacokinetic.

 

物理化学性质&存储条件

分子量 515.9545
分子式 C27H25ClF3N3O2
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

DMSO: ≥ 42 mg/mL

Chemical Name/SMILES

Propanamide, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-[[5-(trifluoromethyl)-2-pyridinyl]oxy]-

参考文献

1. Armstrong HE, et al. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2184-7.

2. Fong TM, et al. J Pharmacol Exp Ther. 2007 Jun;321(3):1013-22.

3. Addy C, et al. Cell Metab. 2008 Jan;7(1):68-78.

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