|(5S,8S)-8-(((R)-1-(3,5-双(三氟甲基)苯基)乙氧基)甲基)-8-苯基-1,7-二氮杂螺[4.5]癸烷-2-酮盐酸盐水合物|CsnPharm

CAS No.: 914462-92-3

(5S,8S)-8-(((R)-1-(3,5-Bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-1,7-diazaspiro[4.5]decan-2-one hydrochloride hydrate Catalog No. CSN16098

Synonyms: SCH 619734;Rolapitant HCl;Rolapitant hydrochloride

Rolapitant HCl H2O is a long-acting, selective and competitive NK-1 receptor antagonist.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Rolapitant is potent, selective and CNS penetrant neurokinin NK1 receptor antagonist with Ki value of 0.66nM, much high selective to NK1 over NK2 and NK3 subtypes of >1000-fold. It is usually used as an antiemetic. Rolapitant dose-dependently inhibited GR73632-induced intracellular Ca2+ release with K_b value of 0.17nM in CHO cells expressing the human NK1 receptor. Rolapitant reversed NK1 agonist-induced foot tapping in gerbils following both intravenous and oral administration up to 24 hours at a minimal effective dose of 0.1 mg/kg. It was active at 0.1 and 1 mg/kg in both acute and delayed emesis models in ferrets, respectively.
作用机制Rolapitant is a competitive antagonist.^[1]
动物研究
剂量
Rat: 5 mg/kg - 100 mg/kg^[2] (p.o.) Monkey: 10 mg/kg^[2] (p.o.)

给药途径
p.o.
参考文献

动物研究
剂量	Rat: 5 mg/kg - 100 mg/kg^[2] (p.o.) Monkey: 10 mg/kg^[2] (p.o.)
给药途径	p.o.

[1] Duffy RA, Morgan C, et al. Rolapitant (SCH 619734): a potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8020 mL
- 9.0098 mL
- 18.0196 mL
- 5 mM
- 0.3604 mL
- 1.8020 mL
- 3.6039 mL
- 10 mM
- 0.1802 mL
- 0.9010 mL
- 1.8020 mL

技术信息

CAS号

914462-92-3

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H29ClF6N2O3

运输

蓝冰

分子量

554.95

别名

SCH 619734;Rolapitant HCl;Rolapitant hydrochloride;Rolapitant;brand name: Varubi;SCH619734 hydrochloride hydrate

溶解度

DMSO	100.0 mg/mL (180.2 mM)

动物实验配方

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(5S,8S)-8-(((R)-1-(3,5-Bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-1,7-diazaspiro[4.5]decan-2-one hydrochloride hydrate Catalog No. CSN16098

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