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Gefapixant (citrate)

Gefapixant citrate is an orally active and potent purinergic P2X3 receptor (P2X3R) antagonist, with IC50 values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant citrate can be used for the research of chronic cough and knee osteoarthritis[1][2][3].

Product Specifications

CAS Number

[2310299-91-1]

Product Name Alternative

MK-7264 (citrate) ; AF-219 (citrate)

UNSPSC

12352005

Target

P2X Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

COVID-19-anti-virus

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/gefapixant-citrate.html

Purity

99.23

Solubility

DMSO : 350 mg/mL (ultrasonic)

Smiles

O=C(CC(C(O)=O)(CC(O)=O)O)O.O=S(N)(C1=C(OC)C=C(C(C)C)C(OC2=CN=C(N)N=C2N)=C1)=O

Molecular Formula

C20H27N5O11S

Molecular Weight

545.52

References & Citations

[1]Anthony P. Ford, et al. The therapeutic promise of ATP antagonism at P2X3 receptors in respiratory and urological disorders. Front Cell Neurosci. 2013; 7: 267.|[2]Ford AP, In pursuit of P2X3 antagonists: novel therapeutics for chronic pain and afferent sensitization. Purinergic Signal. 2012 Feb;8 (Suppl 1) :3-26.|[3]Martin Nguyen A, et al. Validation of a visual analog scale for assessing cough severity in patients with chronic cough. Ther Adv Respir Dis. 2021 Jan-Dec;15:17534666211049743.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

P2X3 Receptor

Available Sizes

Curated Selection

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