SKU : MC530596
CAS Number : 168266-90-8
Molecular Formula : C21H23F3N6O | Molecular Weight : 432.44
Synonyms : GR 205171
Quote RequestPurity | NLT 98% |
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Storage | at 20ºC 2 years |
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Chemical Name | Vofopitant |
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CAS Number | 168266-90-8 |
MDL Number | MFCD06199014 |
Molecular Formula | C21H23F3N6O |
Molecular Weight | 432.44 |
Synonyms | GR 205171 |
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].
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