| Bioactivity | Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough[1]. |
| Target | IC50: 25 nM (hP2X3), >24000 nM (hP2X2/3), 92 nM (rP2X3), 1820 nM (rP2X2/3), 126 nM (gpP2X3), 3450 nM (gpP2X2/3) |
| Invitro | Camlipixant (BLU-5937; 500 nM) 阻断 ATP 介导的背根神经节 (DRG) 神经元敏化[1]。 |
| In Vivo | Camlipixant (BLU-5937; 3-30 mg/kg; oral) 减少组胺和 ATP 诱导的豚鼠咳嗽过敏[1]。Camlipixant (BLU-5937; 10-20 mg/kg; i.p.) 与对照动物相比，不会改变味觉知觉[1]。Camlipixant (BLU-5937) 表现出优异的类药物特性，包括良好的口服生物利用度，在人体内预测清除率低，无血脑屏障渗透性，安全性高[1]。 Animal Model: |
| Name | Camlipixant |
| CAS | 1621164-74-6 |
| Formula | C23H24F2N4O4 |
| Molar Mass | 458.46 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Garceau D, Chauret N. BLU-5937: A selective P2X3 antagonist with potent anti-tussive effect and no taste alteration. Pulm Pharmacol Ther. 2019 Jun;56:56-62. |
Camlipixant
CAS: 1621164-74-6 F: C23H24F2N4O4 W: 458.46
Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with
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