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Vestipitant mesylate

Chemical Structure : Vestipitant mesylate

CAS No.: 334476-64-1

Vestipitant mesylate (GW597599;GW 597588B)

Catalog No.: PC-61579Not For Human Use, Lab Use Only.

Vestipitant (GW597599) is a potent, selective, orally active NK1 receptor antagonist with pKi of 9.65.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Vestipitant (GW597599) is a potent, selective, orally active NK1 receptor antagonist with pKi of 9.65; potently blocks Substance P-mediated phosphorylation of ERK; attenuates fear-induced foot-tapping in gerbils, separation-induced distress-vocalizations in guinea pigs, marble-burying behaviour in mice, and displayes anxiolytic actions in rats.

Chemotherapeutic Agents

Phase 2 Discontinued

Physicochemical Properties

M.Wt 587.554
Formula C24H28F7N3O4S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S)-N-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl]-2-(4-fluoro-2-methylphenyl)-N-methylpiperazine-1-carboxamide mesylate

References

1. Di Fabio R, et al. J Med Chem. 2009 May 28;52(10):3238-47.

2. Brocco M, et al. Eur Neuropsychopharmacol. 2008 Oct;18(10):729-50.

3. Ratti E, et al. Sleep. 2013 Dec 1;36(12):1823-30.

4. Poma SZ, et al. J Psychopharmacol. 2014 May;28(5):491-7.

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