Rolapitant HCl

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
250mg	$1160	Check With Us
500mg	$1650	Check With Us
1g	$2475	Check With Us

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Cat #: V3304 CAS #: 914462-92-3 Purity ≥ 98%

Description: Rolapitant HCl (SCH619734; SCH-619734; SCH 619734; Varubi), the hydrochloride salt of Rolapitant, is a CNS penetreable and orally bioavailable antagonist of neurokinin (NK1) receptor (Ki = 0.66 nM) that was approved in 2015 to prevent delayed nausea and vomiting caused by cancer chemotherapy.

References: Duffy RA, et al. Rolapitant (SCH 619734): a potent, selective and orally active neurokininNK1 receptor antagonist with centrally-mediated antiemetic effects inferrets. Pharmacol Biochem Behav. 2012 Jul;102(1):95-100.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	536.94
Molecular Formula	C25H27ClF6N2O2
CAS No.	914462-92-3
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: ≥ 30mg/mLr
	Water: N/Ar
	Ethanol: N/A
SMILES Code	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
Synonyms	Rolapitant HCl; SCH619734; Rolapitant hydrochloride; SCH-619734; SCH 619734; trade name: Varubi.

Protocol	In Vitro	Rolapitant hydrochloride hydrate is more than 2-fold selective for human NK3 and NK1000 subtypes and has a better affinity for human, guinea pig, gerbil, and monkey NK1 receptors than rats, mice, and rabbits
	In Vivo	Rolapitant hydrochloride hydrate (0.03-1 mg/kg for PO, 0.3-1 mg/kg for IV; single dosage) attenuates GR-73632 (HY-P1192)-induced foot percussion response in Mongolian gerbils
	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)
	Dosages	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

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	1.8624 mL	9.3120 mL	18.6241 mL	37.2481 mL
5mM	0.3725 mL	1.8624 mL	3.7248 mL	7.4496 mL
10mM	0.1862 mL	0.9312 mL	1.8624 mL	3.7248 mL
20mM	0.0931 mL	0.4656 mL	0.9312 mL	1.8624 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.