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首页-小分子抑制剂&激动剂-GPCR-Cannabinoid Receptor-RNB-61
RNB-61

Chemical Structure : RNB-61

CAS No.: 1217403-51-4

RNB-61 (RNB61)

货号: PC-22602Not For Human Use, Lab Use Only.

RNB-61 is a highly potent, selective and orally bioavailable cannabinoid CB2 receptor (CB2R) full agonist with Ki of 0.57/1.33 nM for hCB2R/mCB2R, >5000-fold selective over hCB1R.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

RNB-61 is a highly potent, selective and orally bioavailable cannabinoid CB2 receptor (CB2R) full agonist with Ki of 0.57/1.33 nM for hCB2R/mCB2R, >5000-fold selective over hCB1R.
RNB-61 inhibits the FSK-induced cAMP formation on human CB2R with EC50 of 0.31 nM, and EC50 of 0.29 nM for Q63R human variant.
RNB-61 inhibits the FSK-induced cAMP formation on mouse, rat, dog, and monkey CB2Rs with EC50 values ranging from 0.13 to 1.86 nM.
RNB-61 (0.3-3 mg/kg) exerts protective effects in kidney ischemia reperfusion (I/R) and unilateral ureteral obstruction (UUO) rodent models.

物理化学性质&存储条件

分子量 481.56
分子式 C25H34F3N3O3
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

(E)-N-(5-(tert-butyl)-2-(cyclobutylmethyl)-1-methyl-1,2-dihydro-3H-pyrazol-3-ylidene)-2-(2-hydroxy-2-methylpropoxy)-5-(trifluoromethyl)benzamide

参考文献

1. Patent US20100076029A1.

2. Chicca A, et al. bioRxiv [Preprint]. 2024 Apr 29:2024.04.26.591311.

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