tcsc0003109 Vofopitant

Order Now

AVAILABLE SIZES

$500.00 ORDERING INFORMATION International
TAICLONE BIOTECH CORP.
order@taiclone.com
+886-2-2735-9682
+886-2-2735-9807

Data sheet

Download PDF Datasheet

Technical Inquries

Submit Review

Product Description

Vofopitant is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively.

IC50 & Target: pKi: 10.6 (Human NK1 receptor), 9.5 (Rat NK1 receptor), 9.8 (Ferret NK1 receptor)[1]

In Vitro: Vofopitant is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively. Vofopitant less potently inhibits rat 5-HT1A, bovine 5-HT1D, rat 5-HT2A, rat Histamine H1, guinea-pig Histamine H2 and rat Ca2+ channel, with pKis of 6.3, 6.6, 6.5, 6.5, 6.6, and 5.6, respectively. Vofopitant shows negligible affinity at NK2 and NK3, with pIC50 of <5.0[1]. GR205171 (300 µM) potentiates the effects of paroxetine on cortical [5-HT]ext, and inhibits paroxetine-induced increase in [5-HT]ext in the dorsal raphe nucleus[3].

In Vivo: Vofopitant (GR205171, 30 mg/kg, s.c.) increases the number of choices of the 25-s delayed reward in a T-maze[2]. Vofopitant (GR205171, 30 mg/kg, i.p.) increases the extracellular 5-HT levels in the frontal cortex of paroxetine-treated wild-type mice, rather than in wild-type mice and paroxetine-treated NK1 receptor knockout mice[3].

Information

CAS No168266-90-8
FormulaC21H23F3N6O
Clinical Informationclinicalinformation
PathwayNeuronal Signaling
GPCR/G Protein
TargetNeurokinin Receptor
Neurokinin Receptor

Specifications

Purity / Grade>98%
Solubility10 mM in DMSO
Smilessmiles

Misc Information

Alternative NamesGR 205171
Observed Molecular Weight432.44
Get valuable resources and offers directly to your email.