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Rolapitant

Cat. No. M9019

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Rolapitant Structure
Synonym:

SCH 619734

Size Price Availability Quantity
5mg USD 85  USD85 In stock
10mg USD 135  USD135 In stock
25mg USD 240  USD240 In stock
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Quality Control & Documentation
Biological Activity

Rolapitant (SCH619734) is an orally bioavailable, centrally-acting, selective neurokinin 1 receptor (NK1-receptor) antagonist with a Ki of 0.66 nM. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). Rolapitant is active at 0.1 and 1 mg/kg in both acute and delayed emesis models in ferrets, respectively.

Chemical Information
Molecular Weight 500.48
Formula C25H26F6N2O2
CAS Number 552292-08-7
Solubility (25°C) DMSO ≥ 25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Rapoport B, et al. Eur J Cancer. Efficacy and safety of rolapitant for prevention of chemotherapy-induced nausea and vomiting over multiple cycles of moderately or highly emetogenic chemotherapy.

[2] Rapoport B, et al. Support Care Cancer. 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).

[3] Duffy RA, et al. Pharmacol Biochem Behav. Rolapitant (SCH 619734): a potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets.

Related Neurokinin Receptor Products
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Aprepitant (Emend) is an antiemetic chemical compound that belongs to a class of compounds called substance P antagonists (SPA).

Maropitant

Maropitant (Cerenia) is a novel, selective neurokinin type-1 (NK1) receptor antagonist.

Eprazinone dihydrochloride

Eprazinone is a mucolytic.

Fosaprepitant dimeglumine salt

Fosaprepitant is a water-soluble phosphoryl procompound for Aprepitant which is a NK1 antagonist.*The compound is unstable in solutions, freshly prepared is recommended

Netupitant

Netupitant is a selective neurokinin 1 (NK1) receptor antagonist with potential antiemetic activity with Ki of 0.95 nM.

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Keywords: Rolapitant, SCH 619734 supplier, Neurokinin Receptor, inhibitors, activators

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