Chemical Structure : Vofopitant dihydrochloride
CAS No.:
168266-51-1
Vofopitant dihydrochloride
(GR 205171A)
Catalog No.: PC-23398Not For Human Use, Lab Use Only.
Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [3H]SP binding to the NK1 receptor with pKi values of 9.5 and 10.6 in rat and human membranes respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [3H]SP binding to the NK1 receptor with pKi values of 9.5 and 10.6 in rat and human membranes respectively.
Vofopitant prevents vagal stimulation-induced retching but not neuronal transmission from emetic vagal afferents to solitary nucleus neurons in dogs.
Vofopitant exhibits an acute response to cisplatin but does not vomit during the delayed phase.
Physicochemical Properties
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M.Wt
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505.37
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Formula
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C21H25Cl2F3N6O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(2S,3S)-N-(2-Methoxy-5-(5-(trifluoromethyl)-1H-tetrazol-1-yl)benzyl)-2-phenylpiperidin-3-amine dihydrochloride
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References
1. Gardner CJ, et al. Regul Pept. 1996 Aug 27;65(1):45-53.
2. Gobert A, et al. Neuropsychopharmacology. 2009 Mar;34(4):1039-56.
3. Heldt SA, et al. Behav Pharmacol. 2009 Oct;20(7):584-95.
4. Malik NM, et al. Eur J Pharmacol. 2007 Jan 26;555(2-3):164-73.
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