货号	规格	价格	上海	北京	珠海	重庆	武汉
V43427-1mg	≥98%	￥890.00 V43427-1mg ￥890.00 3-5天	0 货期：3-5天	-	-	-	-
V43427-5mg	≥98%	￥1990.00 V43427-5mg ￥1990.00 3-5天	0 货期：3-5天	-	-	-	-
V43427-10mg	≥98%	￥3490.00 V43427-10mg ￥3490.00 3-5天	0 货期：3-5天	-	-	-	-
V43427-25mg	≥98%	￥6270.00 V43427-25mg ￥6270.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment.

靶点：

NK1R:10.2 (pKi)

体外研究：

Orvepitant (Compound 3a; 0.3-10 mg/kg; Oral administration; marmoset) treatment shows a dose dependant reduction of the number of postures was observed at 1 mg/kg (34.9% reduction), 3 mg/kg (36.6% reduction) and 10 mg/kg (46.4% reduction), suggesting a potential anxiolytic-like effect of the compound[1].
Orvepitant (compound 3a) shows an oral bioavailability (F) of 17% in rat and 55% in dog, plasma clearance (Clp) of 29 mL/min/kg in rat and 6 mL/min/kg in dog and a half-life of 2.3 h in rat and 6.1 h in dog. As far as the brain penetration in rats is concerned, a B/P ratio of 1.2 is observed 5 min after the i.v. administration of a 1 mg/kg dose of Orvepitant[1].

体内研究：

Orvepitant (Compound 3a) is further characterized in terms of the ability to functionally inhibit substance P (SP)-induced release of cytosolic Ca2+ in human neurokinin-1 receptor (hNK1)-CHO cells. Orvepitant (0.3-10 nM), pre-incubated for 1 h at 37℃ before adding the agonist SP, produces a non-surmountable antagonism of agonist concentration-response curve. For Orvepitant apparents pKB value of 10.30.

参考文献：

1. Di Fabio R, et al. Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate. Bioorg Med Chem. 2013 Nov 1;21(21):6264-73.
2. Smith J, et al. The Neurokinin-1 Receptor Antagonist Orvepitant Is a Novel Antitussive Therapy for Chronic Refractory Cough: Results From a Phase 2 Pilot Study (VOLCANO-1). Chest. 2020 Jan;157(1):111-118.

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.343 ml	6.714 ml	13.428 ml
5 mM	0.269 ml	1.343 ml	2.686 ml
10 mM	0.134 ml	0.671 ml	1.343 ml
50 mM	0.027 ml	0.134 ml	0.269 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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