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GR 94800 acetate

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GR 94800 acetate is a potent and selective neurokinin 2(NK-2) antagonist.
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Description GR 94800 acetate is a potent and selective neurokinin 2(NK-2) antagonist.
In vitro GR 94800 在大鼠胃底、结肠、膀胱和输精管这四种组织中展现了高亲和力(pIC50 8.4-9.5),且在这些组织间的效能没有显著差异[3]。
Target activity NK3:6.0(pKb), NK2:9.6(pKb), NK1:6.4(pKb)
Synonyms GR 94800 acetate (141636-65-9 free base)
molecular weight 964.12
Molecular formula C51H65N9O10
Storage keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
References 1. A B McElroy, et al. Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor. J Med Chem. 1992 Jul 10;35(14):2582-91. 2. Stephen D Tichenor, et al. Excitatory motor innervation in the canine rectoanal region: role of changing receptor populations. Br J Pharmacol. 2002 Dec;137(8):1321-9. 3. M A Matuszek, et al. An investigation of tachykinin NK2 receptor subtypes in the rat. Eur J Pharmacol. 1998 Jul 3;352(1):103-9.