A potent NK1 receptor antagonist (Ki = 0.66 nM for the human receptor); greater than 1

Rolapitant – 5 mg

Brand:
Cayman
CAS:
552292-08-7
Storage:
-20
UN-No:
Non-Hazardous - /

Rolapitant is a potent neurokinin-1 (NK1) receptor antagonist (Ki = 0.66 nM for the human receptor).{35201} It is greater than 1,000-fold selective for NK1 over NK2 and NK3 and lacks activity in a panel of 100 receptors, transporters, enzymes, and ion channels. Rolapitant inhibits GR-73632-induced calcium efflux in CHO cells expressing human NK1 in a concentration-dependent manner. In vivo, rolapitant inhibits GR-73632-induced foot-tapping in gerbils (ID90 = 0.3 mg/kg). It also prevents emesis in ferrets induced by apomorphine (Item No. 16094) and cisplatin (Item No. 13119) with ED50 values of 0.03 and 0.07 mg/kg, respectively. Formulations containing rolapitant have been used to prevent chemotherapy-induced nausea and vomiting.  

 

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SKU: 23906 - 5 mg Category:

Description

A potent NK1 receptor antagonist (Ki = 0.66 nM for the human receptor); greater than 1,000-fold selective for NK1 over NK2 and NK3 and lacks activity in a panel of 100 receptors, transporters, enzymes, and ion channels; prevents apomorphine- and cisplatin-induced emesis in ferrets (ED50s = 0.03 and 0.07 mg/kg, respectively)

Formal name: (5S,8S)-8-[[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one

Synonyms: 

Molecular weight: 500.5

CAS: 552292-08-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Pain Research

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