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Vofopitant
CAS No. 168266-90-8
Vofopitant( —— )
Catalog No. M33168 CAS No. 168266-90-8
Vofopitant (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 152 | Get Quote |
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| 5MG | 235 | Get Quote |
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| 10MG | 349 | Get Quote |
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| 25MG | 547 | Get Quote |
|
| 50MG | 793 | Get Quote |
|
| 100MG | 1044 | Get Quote |
|
| 500MG | 2088 | Get Quote |
|
| 1G | Get Quote | Get Quote |
|
Biological Information
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Product NameVofopitant
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NoteResearch use only, not for human use.
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Brief DescriptionVofopitant (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD).
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DescriptionVofopitant is potent tachykinin NK1 receptor antagonist, with pKis of 10.6, 9.5, and 9.8 for human, rat and ferret NK1 receptor, respectively.
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In VitroVofopitant 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. 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.
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In VivoVofopitant (GR205171, 30 mg/kg, s.c.) increases the number of choices of the 25-s delayed reward in a T-maze. 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.
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Synonyms——
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PathwayGPCR/G Protein
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TargetNeurokinin Receptor
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RecptorNeurokinin receptor
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Research Area——
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Indication——
Chemical Information
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CAS Number168266-90-8
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Formula Weight432.44
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Molecular FormulaC21H23F3N6O
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Purity>98% (HPLC)
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Solubility——
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SMILESC(F)(F)(F)C=1N(N=NN1)C2=CC(CN[C@@H]3[C@@H](NCCC3)C4=CC=CC=C4)=C(OC)C=C2
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Gardner CJ, et al. GR205171: a novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity. Regul Pept. 1996 Aug 27;65(1):45-53.?
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