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Gefapixant
CAS No. 1015787-98-0
Gefapixant( AF-219 | MK-7264 )
Catalog No. M10082 CAS No. 1015787-98-0
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).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 49 | In Stock |
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| 5MG | 80 | In Stock |
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| 10MG | 115 | In Stock |
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| 25MG | 237 | In Stock |
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| 50MG | 383 | In Stock |
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| 100MG | 565 | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameGefapixant
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NoteResearch use only, not for human use.
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Brief DescriptionGefapixant (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).
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DescriptionGefapixant (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.
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In VitroGefapixant 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).
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In VivoGefapixant (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).
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SynonymsAF-219 | MK-7264
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PathwayMembrane Transporter/Ion Channel
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TargetP2X Receptor
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RecptorrecombinanthP2X3homotrimers|hP2X2/3heterotrimericreceptors
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Research AreaInflammation/Immunology
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IndicationAsthma
Chemical Information
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CAS Number1015787-98-0
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Formula Weight353.397
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Molecular FormulaC14H19N5O4S
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Purity>98% (HPLC)
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SolubilityDMSO: 10 mM （(< 1 mg/ml )
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SMILESO=S(C1=CC(OC2=CN=C(N)N=C2N)=C(C(C)C)C=C1OC)(N)=O
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Chemical Name5-[(2,4-diaminopyrimidin-5-yl)oxy]-2-methoxy-4-(propan-2-yl)benzene-1-sulfonamide
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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.
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