產(chǎn)品目錄

規(guī)格	5mg 10mg 50mg 100mg 200mg
CAS	177707-12-9
別名	N/A
化學(xué)名	N/A
分子式	C31H24ClF6N3O2
分子量	619.98
溶解度	DMSO: 100 mg/mL (161.30 mM); H2O: < 0.1 mg/mL (insoluble)
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo. IC50 value: 2.6 nMTarget: NK-1 receptorIn vitro, the binding of NKP608 to bovine retina was characterized by an IC50 of 2.6+/-0.4 nM, whereas the compound's affinity to other receptor binding sites, including NK-2 and NK-3, was much lower. Species differences in IC(50) values with NKP608 were less pronounced than with previously described NK-1 receptor antagonists, being 13+/-2 and 27+/-2 nM in gerbil midbrain and rat striatum, respectively. In vivo, using the hind foot thumping model in gerbils, NKP608 exhibited a potent NK-1 antagonistic activity following oral administration (ID(50)=0.23 mg/kg; 2 h pretreatment), supporting a central activity of NKP608. NKP608 may prove a useful anxiolytic compound.

[1]. El-Hashim AZ, Wyss D, Lewis C. Effect of a novel NK1 receptor selective antagonist (NKP608) on citric acid induced cough and airway obstruction. Pulm Pharmacol Ther. 2004;17(1):11-8. [2]. Vendruscolo LF, Takahashi RN, Brüske GR, Ramos A. Evaluation of the anxiolytic-like effect of NKP608, a NK1-receptor antagonist, in two rat strains that differ in anxiety-related behaviors. Psychopharmacology (Berl). 2003 Nov;170(3):287-93. [3]. Rupniak NM, Carlson EJ, Shepheard S, et al. Comparison of the functional blockade of rat substance P (NK1) receptors by GR205171, RP67580, SR140333 and NKP-608. Neuropharmacology. 2003 Aug;45(2):231-41. [4]. Gentsch C, Cutler M, Vassout A, et al. Anxiolytic effect of NKP608, a NK1-receptor antagonist, in the social investigation test in gerbils. Behav Brain Res. 2002 Jul 18;133(2):363-8. [5]. Vassout A, Veenstra S, Hauser K, et al. NKP608: a selective NK-1 receptor antagonist with anxiolytic-like effects in the social interaction and social exploration test in rats. Regul Pept. 2000 Dec 22;96(1-2):7-16.

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1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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