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Orvepitant (maleate)

Orvepitant maleate (GW823296 maleate) is potent, selective, orally active and well-tolerated neurokinin-1 receptor (NK-1) antagonist with a pKi of 10.2 for human neurokinin-1 receptor. Orvepitant maleate can across the blood-brain barrier. Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatment[1][2].

Product Specifications

CAS Number

[579475-24-4]

Product Name Alternative

GW823296 (maleate)

UNSPSC

12352005

Hazard Statement

H302, H361

Target

Neurokinin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/orvepitant-maleate.html

Concentration

10mM

Purity

99.99

Solubility

DMSO : 30 mg/mL (ultrasonic)

Smiles

O=C(N1[C@@H](C2=CC=C(F)C=C2C)C[C@@H](N3C[C@@](CCC4=O)([H])N4CC3)CC1)N([C@@H](C5=CC(C(F)(F)F)=CC(C(F)(F)F)=C5)C)C.O=C(O)/C=C\C(O)=O

Molecular Formula

C35H39F7N4O6

Molecular Weight

744.70

Precautions

H302, H361

References & Citations

[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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Isoform

NK1R

Available Sizes

Curated Selection

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