PKM-833 | FAAH inhibitor | Probechem Biochemicals

Chemical Structure : PKM-833

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PKM-833 (PKM833)

货号: PC-72178Not For Human Use, Lab Use Only.

PKM-833 (PKM833) is a potent, selective, and orally active FAAH inhibitor with IC50 of 8.8 and 10 nM against human and rat FAAH, respectively.

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生物&药学活性

PKM-833 (PKM833) is a potent, selective, and orally active FAAH inhibitor with IC50 of 8.8 and 10 nM against human and rat FAAH, respectively.
PKM‐833 showed human and rat K inact/K i values with 34 300 ± 10 800 and 128 000 ± 39 800 mol-1 L−1 s-1, respectively.
PKM-833 does not inhibit human MAGL and a panel of 137 molecular targets, exhibits weak inhibitory effects (>50%) in five receptor binding assays [PFA, 5‐HT2B, sigma, Na+ channel and Cl‐ channel (GABA gated) at 20 uM.
PKM-833 showed excellent brain penetration and good oral bioavailability, and elevated anandamide (AEA) concentrations in the rat brain.
PKM-833 significantly attenuated formalin-induced pain responses (3 mg/kg) and improved mechanical allodynia in CFA-induced inflammatory pain (0.3-3 mg/kg) in rat models, without significant side effects on catalepsy and motor coordination up to 30 mg/kg.

物理化学性质&存储条件

分子量	407.397
分子式	C19H20F3N5O2
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	(R)-N-(pyridazin-3-yl)-4-(7-(trifluoromethyl)chroman-4-yl)piperazine-1-carboxamide

参考文献

1. Toshiya Endo, et al. Pharmacol Res Perspect. 2020 Apr;8(2):e00569.

PKM-833 (PKM833)

生物&药学活性

物理化学性质&存储条件

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PKM-833 (PKM833)

生物&药学活性

物理化学性质&存储条件

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