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Rolapitant hydrochloride

Catalog No. T3724 CAS 858102-79-1

Synonyms: Rolapitant HCl

Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a K i of 0.66 nM. Rolapitant hydrochloride (Rolapitant HCl) does not interact with CYP3A4. Rolapitant hydrochloride shows potent centrally-mediated anti-emetic activity in both acute and delayed ferret emesis models [1] [2].

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Rolapitant hydrochloride Chemical Structure

Rolapitant hydrochloride, CAS 858102-79-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 258.00
5 mg	In stock	$ 642.00
10 mg	In stock	$ 913.00
25 mg	In stock	$ 1,370.00
50 mg	In stock	$ 1,850.00
100 mg	In stock	$ 2,500.00
1 mL * 10 mM (in DMSO)	In stock	$ 773.00

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Purity: 99.79%

Purity: 98.46%

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Description	Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a K i of 0.66 nM. Rolapitant hydrochloride (Rolapitant HCl) does not interact with CYP3A4. Rolapitant hydrochloride shows potent centrally-mediated anti-emetic activity in both acute and delayed ferret emesis models [1] [2].
In vitro	In vitro studies indicate that rolapitant has a high affinity for the human NK1 receptor of 0.66 nM and high selectivity over the human NK2 and NK3 subtypes of >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, administered orally (0.03-1 mg/kg) or intravenously (0.3-1 mg/kg) as a single dose, effectively mitigates the GR-73632-induced foot-tapping in Mongolian Gerbils and prevents acute emesis triggered by apomorphine and cisplatin in ferrets, with observations lasting up to 72 hours. In the Mongolian Gerbil model, the compound, when given orally, significantly reduces the foot-tapping response, achieving an ID90 at 0.3 mg/kg and maintaining inhibition for over 24 hours. Intravenous administration resulted in a complete cessation of foot-tapping at a dose of 1 mg/kg. In ferrets, rolapitant dose-dependently inhibits vomiting and retching induced by both emetic agents over a 72-hour period, illustrating its potential as an effective clinical antiemetic. This aligns with the ferret emesis model's predictive value for clinical antiemetic efficacy, endorsing rolapitant as a promising candidate for this purpose.

Synonyms	Rolapitant HCl
Molecular Weight	536.94
Formula	C25H27ClF6N2O2
CAS No.	858102-79-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (93.12 mM)

References and Literature

1. Rapoport B, Schwartzberg L, Chasen M, Powers D, Arora S, Navari R, Schnadig I. Eur J Cancer. 2016 Apr;57:23-30. 2. Rapoport B, Chua D, Poma A, Arora S, Wang Y, Fein LE.Support Care Cancer. 2015 Nov;23(11):3281-8.

Citations

1. Sanders D W, Jumper C C, Ackerman P J, et al. SARS-CoV-2 requires cholesterol for viral entry and pathological syncytia formation. Elife. 2021, 10: e65962.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Inhibitor Library GPCR Compound Library EMA Approved Drug Library FDA-Approved Drug Library FDA-Approved & Pharmacopeia Drug Library Neuronal Signaling Compound Library Bioactive Compound Library

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Keywords

Rolapitant hydrochloride 858102-79-1 GPCR/G Protein Neuroscience Neurokinin receptor Rolapitant HCl Rolapitant Hydrochloride inhibitor inhibit

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