Benzenesulfonamide, 5-[(2,4-diamino-5-pyrimidinyl)oxy]-2-methoxy-4-(1-methylethyl)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
- Product Name
- Benzenesulfonamide, 5-[(2,4-diamino-5-pyrimidinyl)oxy]-2-methoxy-4-(1-methylethyl)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
- CAS No.
- 2310299-91-1
- Chemical Name
- Benzenesulfonamide, 5-[(2,4-diamino-5-pyrimidinyl)oxy]-2-methoxy-4-(1-methylethyl)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
- Synonyms
- Gefapixant citrate;Gefapixant Citrat;Jifa Pisheng Citrate;methoxy-4-(1-methylethyl)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1);Benzenesulfonamide, 5-[(2,4-diamino-5-pyrimidinyl)oxy]-2-methoxy-4-(1-methylethyl)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
- CBNumber
- CB19319045
- Molecular Formula
- C20H27N5O11S
- Formula Weight
- 545.52
- MOL File
- 2310299-91-1.mol
Benzenesulfonamide, 5-[(2,4-diamino-5-pyrimidinyl)oxy]-2-methoxy-4-(1-methylethyl)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) Property
- form
- Solid
- color
- White to off-white
- InChIKey
- AIJVJYUOMCRFOE-UHFFFAOYSA-N
- SMILES
- C(O)(C(=O)O)(CC(=O)O)CC(=O)O.O(C1=CN=C(N)N=C1N)C1C=C(S(=O)(=O)N)C(OC)=CC=1C(C)C
Benzenesulfonamide, 5-[(2,4-diamino-5-pyrimidinyl)oxy]-2-methoxy-4-(1-methylethyl)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) Chemical Properties,Usage,Production
Uses
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].
in vivo
Gefapixant citrate (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)[2].
IC 50
P2X3 Receptor
References
[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. DOI:10.3389/fncel.2013.00267
[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. DOI:10.1007/s11302-011-9271-6
[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. DOI:10.1177/17534666211049743
Benzenesulfonamide, 5-[(2,4-diamino-5-pyrimidinyl)oxy]-2-methoxy-4-(1-methylethyl)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Benzenesulfonamide, 5-[(2,4-diamino-5-pyrimidinyl)oxy]-2-methoxy-4-(1-methylethyl)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) manufacturers
- Product
- Gefapixant Citrate 2310299-91-1
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2024-07-24
- Product
- Gefapixant Citrate. 2310299-91-1
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2025-01-07