Rolapitant, CAS 552292-08-7

Formulation: A crystalline solid

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

Purity: ≥98%

Formula Markup: C25H26F6N2O2

Formula Weight: 500,5

Shelf life (days): 1460

CAS Number: 552292-08-7

Notes: 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.

• Artikelnummer: CAY23906-10
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 23906-10
• Green Labware: Nein
• Verpackungseinheit: 10 mg
• Mengeneinheit: STK