Casopitant | NK1R antagonist | Probechem Biochemicals

Chemical Structure : Casopitant

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Casopitant (GW679769, GW 679769)

货号: PC-61580Not For Human Use, Lab Use Only.

Casopitant (GW679769) is a potent, selective, orally active, and brain penetrant neurokinin 1 (NK1) receptor antagonist with pKi of 9.48.

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生物&药学活性

Casopitant (GW679769) is a potent, selective, orally active, and brain penetrant neurokinin 1 (NK1) receptor antagonist with pKi of 9.48.

Casopitant (GW679769) inhibit SP-induced release of cytosolic Ca2+ in h-NK1-CHO cells using FLIPR with pA2 value of 9.7.

Casopitant (GW679769) possesses subnanomolar affinity and high selectivity for the NK1 receptors without sign of pharmacological species difference between human and gerbil NK1 receptors.

Casopitant (GW679769) possesses an anxiolytic-like property, confirming the preclinical profile of NK1 receptor antagonists on emotional behavior.

物理化学性质&存储条件

分子量	616.625
分子式	C30H35F7N4O2
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	(2R,4S)-4-(4-acetylpiperazin-1-yl)-N-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl]-2-(4-fluoro-2-methylphenyl)-N-methylpiperidine-1-carboxamide

参考文献

1. Minthorn E, et al. Drug Metab Dispos. 2008 Sep;36(9):1846-52.

2. Ruhlmann C, et al. Ther Clin Risk Manag. 2009 Apr;5(2):375-84.

3. Singla NK, et al. Anesthesiology. 2010 Jul;113(1):74-82.

Casopitant (GW679769, GW 679769)

生物&药学活性

物理化学性质&存储条件

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Casopitant (GW679769, GW 679769)

生物&药学活性

物理化学性质&存储条件

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