Home Neuronal Signaling Neurokinin Receptor antagonist Rolapitant For research use only.

Rolapitant

Synonyms: SCH-619734

Rolapitant (SCH-619734) is a selective and competitive antagonist of human substance P/NK1 receptors with antiemetic activity. It 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.

Rolapitant Chemical Structure

Rolapitant Chemical Structure

CAS No. 552292-08-7

Purity & Quality Control

Rolapitant Related Products

Biological Activity

Description Rolapitant (SCH-619734) is a selective and competitive antagonist of human substance P/NK1 receptors with antiemetic activity. It 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.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02991456 Completed
Chemo-radiation Induced Nausea and Vomiting
Duke University
 October 9 2017 Phase 2

Chemical Information & Solubility

Molecular Weight 500.48 Formula

C25H26F6N2O2
CAS No. 552292-08-7 SDF --
Smiles CC(C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F)OCC2(CCC3(CCC(=O)N3)CN2)C4=CC=CC=C4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (199.8 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
Batch:

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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