| Company Name: |
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
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| Tel: |
18818260767 |
| Email: |
sales@chemegen.com |
| Products Intro: |
Product Name:P2X3 antagonist 34
CAS:2417288-67-4
Purity:98% Package:10 mg;50 mg;100 mg;500 mg;1 g;5 g;10 g
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| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
4008200310 |
| Email: |
marketing@tsbiochem.com |
| Products Intro: |
Product Name:P2X3 antagonist 34
CAS:2417288-67-4
Purity:98% Package:100 mg；50 mg
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| | 1-Piperidinecarboxylic acid, 3-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (3S)- Basic information |
| Product Name: | 1-Piperidinecarboxylic acid, 3-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (3S)- | | Synonyms: | 1-Piperidinecarboxylic acid, 3-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (3S)- | | CAS: | 2417288-67-4 | | MF: | C24H26F2N4O3 | | MW: | 456.48 | | EINECS: | | | Product Categories: | | | Mol File: | 2417288-67-4.mol | ![1-Piperidinecarboxylic acid, 3-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (3S)- Structure](CAS/20210111/GIF/2417288-67-4.gif) |
| | 1-Piperidinecarboxylic acid, 3-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (3S)- Chemical Properties |
| density | 1.34±0.1 g/cm3(Predicted) | | pka | 13.53±0.46(Predicted) | | form | Solid | | color | Off-white to light yellow |
| | 1-Piperidinecarboxylic acid, 3-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (3S)- Usage And Synthesis |
| Biological Activity | P2X3 antagonist 34 is a potent, selective, orally active P2X3 homotrimeric receptor antagonist with IC50 of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively . It is less active at human, rat and guinea pig P2X2/3 heterotrimeric receptors and has a strong antitussive effect. | | in vitro | P2X3 antagonist 34 (BLU-5937; 500 nM) is able to block αβ-meATP-induced sensitization and firing activity of isolated primary nociceptors in rat dorsal root ganglions (DRGs), through P2X3 homotrimeric receptor antagonism. The sensitizing effect of αβ-meATP and the inhibition of P2X3 antagonist 34 are reversible after washout. | | in vivo | P2X3 antagonist 34 (BLU-5937; 0.3-0 mg/kg, oral administration; male Dunkin Hartley guinea pigs) treatment significantly reduces the histamine-induced enhancement in the number of citric acid-induced coughs in a dose -dependent fashion in a guinea pig cough model.
It (BLU-5937; 3 and 30 mg/kg, oral) is also shown to reduce significantly and dose-dependently the ATP-induced enhancement of citric acid- induced coughs in the guinea pig. < table class="zh_use_1"> | Animal Model: | Male Dunkin Hartley guinea pigs | | Dosage: | 0.3 mg/kg, 3 mg/kg, 30 mg/kg | | Administration: | Oral administration | | Result: | < td class="col2"> Significantly reduced the histamine-induced enhancement in the n umber of citric acid-induced coughs in a dose-dependent fashion. |
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