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Gefapixant(AF219 MK-7264)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Gefapixant(AF219 MK-7264)图片
CAS NO:1015787-98-0
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件

Name: Gefapixant
CAS#: 1015787-98-0
Chemical Formula: C14H19N5O4S
Exact Mass: 353.1158
Molecular Weight: 353.39
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Technical InformationSynonym: AF-219; MK7264; RO4926219; AF219; MK 7264; RO-4926219; AF 219; MK-7264; RO 4926219;
Chemical Name: 5-[(2,4-diaminopyrimidin-5-yl)oxy]-2-methoxy-4-(propan-2-yl)benzene-1-sulfonamide
InChi Key: HLWURFKMDLAKOD-UHFFFAOYSA-N
InChi Code: InChI=1S/C14H19N5O4S/c1-7(2)8-4-10(22-3)12(24(17,20)21)5-9(8)23-11-6-18-14(16)19-13(11)15/h4-7H,1-3H3,(H2,17,20,21)(H4,15,16,18,19)
SMILES Code: O=S(C1=CC(OC2=CN=C(N)N=C2N)=C(C(C)C)C=C1OC)(N)=O
实验参考方法
Target

IC50: ~30 nM (recombinant hP2X3 homotrimers), 100-250 nM (hP2X2/3 heterotrimeric receptors)[1].

In VitroThe aryloxy-pyrimidinediamine, Gefapixant (AF-219) is an orally active small molecule antagonist at human P2X3-containing receptors. The IC50 of Gefapixant has been reported as ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors, potencies very similar to those reported for recombinant rat receptors, and it 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)[1].
In VivoIn an adjuvant-induced rthritis model in rat (7d following intraplantar administration of complete Freund's adjuvant), AF-353 produces dose-dependent antihyperalgesia in weight-bearing asymmetry and von Frey filament mechanical tests; magnitude of effect is compared with that of the NSAID naproxen. In a rat model of knee osteoarthritis (14d following intra-articular administration of monoiodoacetate), Gefapixant (7d bid, orally; right) attenuates the weight bearing laterality with complete reversal of apparent hyperalgesia at the two higher doses[2].
Animal AdminRats[2] A rodent model often employs for assessing potential for drug effect in osteoarthritis (OA) pain is based on intraarticular injection of monoiodoacetate (mIOA) into one knee joint of the rat. Progressive loss of chondrocytes leads to histological changes of the articular cartilage over subsequent weeks that resemble the changes which occur in human OA, leading to joint discomfort exemplified by a shift in the weight distribution (asymmetry) to favor the unaffected limb. To measure the effect of Gefapixant on the weight bearing laterality and apparent hyperalgesia, Gefapixant is given by intraplantar or oral administration to the rats, with different concentrations (6, 20, and 60 mg/kg) two times a day and continues up to a week[2].
References[1]. The therapeutic promise of ATP antagonism at P2X3 receptors in respiratory and urological disorders. Front Cell Neurosci. 2013; 7: 267.

[2]. In pursuit of P2X3 antagonists: novel therapeutics for chronic pain and afferent sensitization. Purinergic Signal. 2012 Feb;8(Suppl 1):3-26