Rolapitant (hydrochloride hydrate)
CAS No. : 914462-92-3
(Synonyms: SCH619734 (hydrochloride hydrate))
| Size | Price | Stock |
|---|---|---|
| 5mg | $60 | In-stock |
| 10mg | $96 | In-stock |
| 25mg | $195 | In-stock |
| 50mg | $320 | In-stock |
| 100mg | $520 | In-stock |
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| Cat. No. : | HY-16436 |
| M.Wt: | 554.95 |
| Formula: | C25H29ClF6N2O3 |
| Purity: | >98 % |
| Solubility: | DMSO : 250 mg/mL (ultrasonic) |
Rolapitant hydrochloride hydrate (SCH619734 hydrochloride hydrate) is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride hydrate does not interact with CYP3A4. Rolapitant hydrochloride hydrate shows potent anti-emetic activity in a ferret emesis model[1][2].
IC50 & Target:Ki: 0.66 nM (neurokinin)[1]
In Vitro:Rolapitant hydrochloride hydrate 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 hydrochloride hydrate (1-1000 nM) inhibits the GR-73632 (an NK1 receptor agonist)-induced calcium efflux in a concentration-dependent and competitive manner in CHO cells expressing the human NK1 receptor[1].
In Vivo:Rolapitant hydrochloride hydrate (0.03-1 mg/kg for PO, 0.3-1 mg/kg for IV; single dosage) attenuates the GR-73632 (HY-P1192)-induced foot-tapping response in Mongolian Gerbils[1].
Rolapitant hydrochloride hydrate (0.03-1 mg/kg; PO; single dosage; observed for 72 h) blocks acute emesis induced by both apomorphine and cisplatin (HY-17394) in ferrets[1].
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