2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. Rolapitant hydrochloride

Rolapitant hydrochloride  (Synonyms: SCH619734 hydrochloride)

Cat. No.: HY-14751A
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Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride does not interact with CYP3A4. Rolapitant hydrochloride shows potent anti-emetic activity in a ferret emesis model.

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Rolapitant hydrochloride Chemical Structure

Rolapitant hydrochloride Chemical Structure

CAS No. : 858102-79-1

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Rolapitant hydrochloride Related Antibodies

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Description

Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a Ki of 0.66 nM. Rolapitant hydrochloride does not interact with CYP3A4. Rolapitant hydrochloride shows potent anti-emetic activity in a ferret emesis model[1][2].

IC50 & Target[1]

human NK1

0.66 (Ki)

gerbil NK1

0.13 (Ki)

guinea pig NK1

0.72 (Ki)

monkey NK1

2.5 (Ki)

rabbit NK1

31.7 (Ki)

rat NK1

78.6 (Ki)

mouse NK1

60.4 (Ki)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Rolapitant hydrochloride Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

536.94

Formula

C25H27ClF6N2O2
CAS No.
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.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Rolapitant hydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rolapitant858102-79-1SCH619734SCH 619734SCH-619734Neurokinin ReceptorNK receptorTachykinin receptorlong-actingorally activeanti-emeticemesisferretMongolian Gerbilsfoot tappingretchesvomitsInhibitorinhibitorinhibit

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