For research use only. Not for therapeutic Use.
Rolapitant (Cat No.:I009177), also known as SCH-619734, is a long-term, selective and oral neurokinin-1 (NK1) receptor antagonist with potential antiemetic activity, Ki value of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant showed strong antiemetic activity in the ferret vomiting model.
| Catalog Number | I009177 |
| CAS Number | 552292-08-7 (free base) |
| Synonyms | Rolapitant free base; SCH619734 SCH-619734; SCH 619734; brand name: Varubi.;(5S,8S)-8-(((R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-1,7-diazaspiro[4.5]decan-2-one |
| Molecular Formula | C25H26F6N2O2 |
| Purity | ≥95% |
| Target | NK1-receptor antagonist |
| Solubility | Soluble in DMSO |
| Storage | 0 - 4 °C for short term, or -20 °C for long term |
| InChI | InChI=1S/C25H26F6N2O2/c1-16(17-11-19(24(26,27)28)13-20(12-17)25(29,30)31)35-15-23(18-5-3-2-4-6-18)10-9-22(14-32-23)8-7-21(34)33-22/h2-6,11-13,16,32H,7-10,14-15H2,1H3,(H,33,34)/t16-,22-,23-/m1/s1 |
| InChIKey | FIVSJYGQAIEMOC-ZGNKEGEESA-N |
| SMILES | O=C1N[C@]2(CN[C@@](C3=CC=CC=C3)(CO[C@@H](C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)C)CC2)CC1 |
| Reference | </br> 1:Rapoport B, Schwartzberg L, Chasen M, Powers D, Arora S, Navari R, Schnadig I. Efficacy and safety of rolapitant for prevention of chemotherapy-induced nausea and vomiting over multiple cycles of moderately or highly emetogenic chemotherapy. Eur J Cancer. 2016 Apr;57:23-30. doi: 10.1016/j.ejca.2015.12.023. PubMed PMID: 26851398.</br> 2: Rapoport B, Chua D, Poma A, Arora S, Wang Y, Fein LE. Study of rolapitant, a novel, long-acting, NK-1 receptor antagonist, for the prevention of chemotherapy-induced nausea and vomiting (CINV) due to highly emetogenic chemotherapy (HEC). Support Care Cancer. 2015 Nov;23(11):3281-8. doi: 10.1007/s00520-015-2738-1. PubMed PMID: 25940030. |
