Rolapitant Hydrochloride Monohydrate NEW
| Price | $6 | $4 | $2 |
| Package | 1kg | 10kg | 100kg |
| Min. Order: | 1kg |
| Supply Ability: | 100kg |
| Update Time: | 2025-08-06 |
Product Details
| Product Name: Rolapitant Hydrochloride Monohydrate | CAS No.: 914462-92-3 |
| Min. Order: 1kg | Purity: 99% |
| Supply Ability: 100kg | Release date: 2025/08/06 |
| Lead time: in stock | Packaging: bag/bottle/drum//IBC, as request |
| Delivery: By sea, by air, by express | Origin: Manufacturer, advantage products |
| COA, MSDS: Available, contact us for details | Contact: Tina |
PRODUCT INFORMATION
| Common Name | Rolapitant Hydrochloride Monohydrate | ||
|---|---|---|---|
| CAS Number | 914462-92-3 | Molecular Weight | 554.953 |
| Density | N/A | Boiling Point | N/A |
| Molecular Formula | C25H29ClF6N2O3 | Melting Point | N/A |
| MSDS | N/A | Flash Point | N/A |
| Purity | Quantity | Budget | Inquiry |
|---|
Use of Rolapitant Hydrochloride MonohydrateRolapitant 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]. |
| Name | (5S,8S)-8-[[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]methyl]-8-phenyl-1,9-diazaspiro[4.5]decan-2-one,hydrate,hydrochloride |
|---|---|
| Synonym | More Synonyms |
| Description | 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]. |
|---|---|
| Related Catalog | Research Areas >> Cancer Signaling Pathways >> Neuronal Signaling >> Neurokinin Receptor Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> Neurokinin Receptor |
| Target | human NK1:0.66 nM (Ki) gerbil NK1:0.13 nM (Ki) guinea pig NK1:0.72 nM (Ki) monkey NK1:2.5 nM (Ki) rabbit NK1:31.7 nM (Ki) rat NK1:78.6 nM (Ki) mouse NK1:60.4 nM (Ki) |
| In Vitro | |
| In Vivo | Rolapitant hydrochloride hydrate (0.03-1 mg/kg for PO, 0.3-1 mg/kg for IV; single dosage) [1]。 Rolapitant hydrochloride hydrate (0.03-1 mg/kg; PO; single dosage; observed for 72 h) [1]。 Animal Model: Female Mongolian Gerbils (30-60 g; anesthetized by inhalation of an oxygen:isofluorane mixture after 4 h PO or immediately after IV, then injected with 5 μl of 3 pmol solution of GR-73632 via ICV)[1] Dosage: 0.03, 0.1, 0.3 and 1 mg/kg for PO, 0.3 and 1 mg/kg for IV Administration: PO or IV, single dosage Result: Attenuated dose-dependently the GR-73632-induced foot-tapping response when administered PO 4 h before testing, with an ID90 of 0.3 mg/kg, and the inhibition in foot tapping for at least 24 h. Blocked dose-dependently the foot tapping induced by GR-73632 when administered IV, with complete blockade observed at 1 mg/kg. Animal Model: Ferrets (treated with subcutaneous administration of 0.125 mg/kg apomorphine or intraperitoneal administration of 10 mg/kg cisplatin)[1] Dosage: 0.03, 0.1, 0.3 and 1 mg/kg Administration: PO; single dosage; observed for 72 h Result: Blocked dose-dependently acute emesis induced by both apomorphine and cisplatin in ferrets. Produced a robust decrease in retches and vomits in ferrets that was maintained throughout the 72 h observation period. |
| References | [1]. Duffy RA, et al. Rolapitant (SCH 619734): a potent, selective and orally active neurokininNK1 receptor antagonist with centrally-mediated antiemetic effects inferrets. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100. [2]. Rapoport B, et al. 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. |
| Molecular Formula | C25H29ClF6N2O3 |
|---|---|
| Molecular Weight | 554.953 |
| Exact Mass | 554.177063 |
| PSA | 63.08000 |
| LogP | 7.07190 |
| rolapitant hydrochloride hydrate |
| Rolapitant hydrochloride |
| UNII:57O5S1QSAQ |
| (5S,8S)-8-({(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy}methyl)-8-phenyl-1,7-diazaspiro[4.5]decan-2-one hydrochloride hydrate |
| Varubi |
| 1,7-Diazaspiro[4.5]decan-2-one, 8-[[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]methyl]-8-phenyl-, (5S,8S)-, hydrochloride, hydrate (1:1:1) |
| UNII-57O5S1QSAQ |
| Rolapitant HCl |
| Rolapitant Hydrochloride Monohydrate |
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Company Profile Introduction
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