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Orvepitant

Chemical Structure : Orvepitant

CAS No.: 579475-18-6

Orvepitant (GW-823296;GW823296)

Catalog No.: PC-61552Not For Human Use, Lab Use Only.

Orvepitant (GW823296) is a potent and selective, brain penetrant NK1 receptor antagonist with pKi of 10.2.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Orvepitant (GW823296) is a potent and selective, brain penetrant NK1 receptor antagonist with pKi of 10.2; exhibits an excellent, dose dependent inhibition of foot tapping in gerbils after oral administration with an ID50 of 0.11 mg/kg; shows antidepressant effects.

Depression

Phase 2 Clinical

Physicochemical Properties

M.Wt 628.623
Formula C31H35F7N4O2
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

(2R,4S)-N-[(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethyl]-2-(4-fluoro-2-methylphenyl)-4-[(8aS)-hexahydro-6-oxopyrrolo[1,2-a]pyrazin-2(1H)-yl]-N-methyl-1-piperidinecarboxamide

References

1. Di Fabio R, et al. Bioorg Med Chem. 2013 Nov 1;21(21):6264-73.

2. Ratti E, et al. J Psychopharmacol. 2013 May;27(5):424-34.

3. Trower MK, et al. Exp Dermatol. 2014 Nov;23(11):858-60.

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