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Orvepitant maleate

Catalog No. T16406 CAS 579475-24-4

Synonyms: GW823296 maleate

Orvepitant maleate is an effective, selective, and well-tolerated neurokinin-1 receptor (NK-1) antagonist (pKi: 10.2 for human neurokinin-1 receptor). Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment. Orvepitant maleate can across the blood-brain barrier.

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Orvepitant maleate, CAS 579475-24-4

Pack Size	Availability	Price/USD
25 mg	10-14 weeks	$ 688.00
50 mg	10-14 weeks	$ 913.00
100 mg	10-14 weeks	$ 1,360.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Orvepitant maleate is an effective, selective, and well-tolerated neurokinin-1 receptor (NK-1) antagonist (pKi: 10.2 for human neurokinin-1 receptor). Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment. Orvepitant maleate can across the blood-brain barrier.
Targets&IC50	NK1:10.2 （pki）
In vitro	Orvepitant (0.3-10 nM), pre-incubated for 1 h at 37℃ before adding the agonist SP, produces a non-surmountable antagonism of agonist concentration-response curve. For the Orvepitant apparent pKB value is 10.30. Orvepitant is further characterized in terms of the ability to functionally inhibit substance P (SP)-induced release of cytosolic Ca2+ in human neurokinin-1 receptor (hNK1)-CHO cells [1].
In vivo	Orvepitant shows an oral bioavailability (F) of 17% in rat and 55% in a dog, plasma clearance (Clp) of 29 mL/min/kg in rat and 6 mL/min/kg in dog and a half-life of 2.3 h in rat and 6.1 h in the dog. Orvepitant (0.3-10 mg/kg; p.o.; marmoset) treatment displays a dose-dependent reduction of the number of postures was observed at 1 mg/kg (34.9% reduction), 3 mg/kg (36.6% reduction) and 10 mg/kg (46.4% reduction), suggesting a potential anxiolytic-like effect of the compound. As far as the brain penetration in rats is concerned, a B/P ratio of 1.2 is observed 5 min after the i.v. administration of a 1 mg/kg dose of Orvepitant[1].

Synonyms	GW823296 maleate
Molecular Weight	744.7
Formula	C35H39F7N4O6
CAS No.	579475-24-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Di Fabio R, et al. Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate. Bioorg Med Chem. 2013 Nov 1;21(21):6264-73. 2. Smith J, et al. The Neurokinin-1 Receptor Antagonist Orvepitant Is a Novel Antitussive Therapy for Chronic Refractory Cough: Results From a Phase 2 Pilot Study (VOLCANO-1). Chest. 2020 Jan;157(1):111-118.

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Keywords

Orvepitant maleate 579475-24-4 GPCR/G Protein Neuroscience Neurokinin receptor Orvepitant Maleate GW823296 Maleate GW 823296 Maleate GW-823296 Maleate GW823296 maleate inhibitor inhibit

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