Rolapitant
CAS No. : 552292-08-7
(Synonyms: SCH619734)
| Size | Price | Stock |
|---|---|---|
| 5mg | $85 | In-stock |
| 10mg | $135 | In-stock |
| 25mg | $240 | In-stock |
| 50mg | $360 | In-stock |
| 100mg | $500 | In-stock |
| 200 mg | Get quote | |
| 500 mg | Get quote | |
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| Cat. No. : | HY-14751 |
| M.Wt: | 500.48 |
| Formula: | C25H26F6N2O2 |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 30 mg/mL |
Rolapitant (SCH619734) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant does not interact with CYP3A4. Rolapitant shows potent anti-emetic activity in a ferret emesis model[1][2].
IC50 & Target:Ki: 0.66 nM (neurokinin)[1]
In Vitro:Rolapitant has high selectivity over the human NK2 and NK3 subtypes of more than 1000-fold, as well as preferential affinity for human, guinea pig, gerbil and monkey NK1 receptors over rat, mouse and rabbit[1].
Rolapitant (1-1000 nM) inhibits the GR-73632 (an NK1 receptor agonist)-induced calcium efflux with a concentration-dependent and competitive manner in CHO cells expressing the human NK1 receptor[1].
In Vivo:Rolapitant (0.03-1 mg/kg for PO, 0.3-1 mg/kg for IV; single dosage) attenuates the GR-73632-induced foot-tapping response in Mongolian Gerbils[1].
Rolapitant (0.03-1 mg/kg; PO; single dosage; observed for 72 h) blocks acute emesis induced by both apomorphine and cisplatin in ferrets[1].
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