AM251 | CB1 antagonist | Probechem Biochemicals

Chemical Structure : AM251

CAS No.: 183232-66-8

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AM251 (AM 251)

货号: PC-20082Not For Human Use, Lab Use Only.

AM251 (AM 251) is a potent, selective CB1 receptor antagonist (inverse agonist) with IC50 of 8 nM, Ki of 7.49 nM, displays 306-fold selectivity over CB2 receptors.

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10 mg	￥780	In stock
25 mg	￥1380	In stock
50 mg	￥2280	In stock
100 mg		Get quote

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生物&药学活性

AM251 (AM 251) is a potent, selective CB1 receptor antagonist (inverse agonist) with IC50 of 8 nM, Ki of 7.49 nM, displays 306-fold selectivity over CB2 receptors.
AM251 also is a potent GPR55 agonist (EC50=39 nM) and μ-opioid receptor antagonist (Ki=251 nM).
AM251 blocked the WIN 55,212-2-induced inhibition of evoked Iinhibitory postsynaptic currents (IPSCs).
Pretreatment with AM 251 (3 mg kg(-1)) antagonized the pressor and vasoconstrictor effects of HU 210 and WIN-55212-2 in conscious rats.

物理化学性质&存储条件

分子量	555.24
分子式	C22H21Cl2IN4O
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	N-(Piperidin-1-yl)-5-(4-iodophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide

参考文献

1. Gatley SJ, et al. Eur J Pharmacol. 1996 Jul 4;307(3):331-8.

2. Diana MA, et al. J Neurosci. 2002 Jan 1;22(1):200-8.

3. Gardiner SM, et al. Br J Pharmacol. 2002 Jun;136(4):581-7.

AM251 (AM 251)

生物&药学活性

物理化学性质&存储条件

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AM251 (AM 251)

生物&药学活性

物理化学性质&存储条件

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