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Rolapitant hydrochloride hydrate

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Catalog No. T68371Cas No. 914462-92-3

Rolapitant, also known as SCH-619734, is an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. 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). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy.

Rolapitant hydrochloride hydrate
Other Forms of Rolapitant hydrochloride hydrate:

Rolapitant hydrochloride hydrate

😃Good
Catalog No. T68371Cas No. 914462-92-3
Rolapitant, also known as SCH-619734, is an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. 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). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy.
Pack SizePriceAvailabilityQuantity
25 mg$2,5701-2 weeks
50 mg$3,3801-2 weeks
100 mg$4,6001-2 weeks
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Product Introduction

Bioactivity
Description
Rolapitant, also known as SCH-619734, is an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. 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). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy.
Targets&IC50
NK1 (mouse):60.4 nM (Ki), NK1 (gerbil):0.13 nM (Ki), NK1 (monkey):2.5 nM (Ki), rat NK1:78.6 nM (Ki), NK1 (human):0.66 nM (Ki), NK1 (rabbit):31.7 nM (Ki), NK1 (guinea pig):0.72 nM (Ki)
Chemical Properties
Molecular Weight554.95
FormulaC25H29ClF6N2O3
Cas No.914462-92-3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
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Keywords

SCH 619734Rolapitant hydrochloride, Rolapitant, brand name: Varubi.Rolapitant hydrochloride HydrateRolapitant HCl
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