Comparison

Rolapitant

Item no. V3303-10mg
Manufacturer InvivoChem LLC
CASRN 552292-08-7
Amount 10 mg
Quantity options 100 mg 250 mg 25 mg 500 mg 50 mg 5 mg
Category
Type Biochemicals
Specific against other
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Available
Description
InvivoChem Cat #:V3303CAS #:552292-08-7 (free base); 914462-92-3 (HCl) Purity >=98%

Description: Rolapitant (formerly known as SCH619734) is a potent, selective, CNS penetrant and orally bioactive neurokinin NK1 receptor antagonist with a Ki of 0.66 nM. NK1 receptor antagonists have been shown to have a variety of physiological and potential therapeutic effects in animal models and in humans. Rolapitant shows behavioral effects in animals models of emesis. 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. Rolapitant is a functionally competitive antagonist, as measured by calcium efflux, with a calculated Kb of 0.17 nM. Rolapitant reversed NK1 agonist-induced foot tapping in gerbils following both intravenous and oral administration up to 24 hours at a minimal effective dose (MED) of 0.1 mg/kg. Rolapitant was active at 0.1 and 1 mg/kg in both acute and delayed emesis models in ferrets, respectively, consistent with clinical data for other NK1 antagonists. Clinical efficacy of anti-emetics is highly correlated with efficacy in the ferret emesis model, suggesting rolapitant is a viable clinical candidate for this indication.

Description:

References: 2012 Jul; 102(1):95-100.

References:


Molecular Weight (MW)
500.49
Formula
C25H26F6N2O2
CAS No.
5552292-08-7 (free base)
Storage
-20C for 3 years in powder form
-80C for 2 years in solvent
Solubility (In vitro)
DMSO: >= 30mg/mL
Water: N/A
Ethanol: N/A
Chemical Name
(5S, 8S)-8-(((R)-1-(3, 5-bis(trifluoromethyl)phenyl)ethoxy)methyl)-8-phenyl-1, 7-diazaspiro[4.5]decan-2-one
Synonyms
SCH619734 SCH-619734; SCH 619734; brand name: Varubi.
SMILES Code
O=C1N[C]2(CN[C](C3=CC=CC=C3)(CO[CH](C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)C)CC2)CC1

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Amount: 10 mg
Available: In stock
available

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