Gefapixant( AF-219 | MK-7264 )

Catalog No. M10082 CAS No. 1015787-98-0

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

Get Quotation Bulk Inquiry Add to Cart

Product Name

Gefapixant
Note

Research use only, not for human use.
Brief Description

Gefapixant (AF-219, MK-7264) is an orally active, small molecule antagonist of P2X3-containing receptor with IC50 of 30 nM (hP2X3 homotrimer) and 100-250 nM (hP2X2/3 heterotrimer).
Description

Gefapixant (AF-219, MK-7264) is an orally active, small molecule antagonist of P2X3-containing receptor with IC50 of 30 nM (hP2X3 homotrimer) and 100-250 nM (hP2X2/3 heterotrimer); displays no inhibitory impact on any non-P2X3 subunit containing receptors (IC50 >10,000 nM at recombinant homotrimeric hP2X1, hP2X2, hP2X4, rP2X5 and hP2X7 channels); markedly and significantly reduced objective cough frequency in clinical trials.Asthma Phase 2 Clinical.
In Vitro

Gefapixant displays no inhibitory impact on any non-P2X3 subunit containing receptors (IC50 values >10,000 nM at recombinant homotrimeric hP2X1, hP2X2, hP2X4, rP2X5 and hP2X7 channels).
In Vivo

Gefapixant (7d bid, orally) attenuates the weight bearing laterality with complete reversal of apparent hyperalgesia at the two higher doses in a rat model of knee osteoarthritis (14d following intra-articular administration of monoiodoacetate).
Synonyms

AF-219 | MK-7264
Pathway

Membrane Transporter/Ion Channel
Target

P2X Receptor
Recptor

recombinanthP2X3homotrimers|hP2X2/3heterotrimericreceptors
Research Area

Inflammation/Immunology
Indication

Asthma

CAS Number

1015787-98-0
Formula Weight

353.397
Molecular Formula

C14H19N5O4S
Purity

>98% (HPLC)
Solubility

DMSO: 10 mM （(< 1 mg/ml )
SMILES

O=S(C1=CC(OC2=CN=C(N)N=C2N)=C(C(C)C)C=C1OC)(N)=O
Chemical Name

5-[(2,4-diaminopyrimidin-5-yl)oxy]-2-methoxy-4-(propan-2-yl)benzene-1-sulfonamide

1. Abdulqawi R, et al. Lancet. 2015 Mar 28;385(9974):1198-205. 2. Ford AP, et al. Front Cell Neurosci. 2013 Dec 19;7:267.

Calculator

molnova catalog