Camlipixant

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Camlipixant (BLU-5937) 是一种有效的、选择性的、非竞争性和具有口服活性的 P2X3 同型三聚体受体拮抗剂，对 hP2X3 同型三聚体的 IC50 为 25 nM。Camlipixant 表现出较强的止咳效果，且无味觉改变。Camlipixant 可用于不明原因、难治性慢性咳嗽的研究。

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.

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Animal Model:Male Dunkin Hartley guinea pigsDosage:0.3, 3, 30 mg/kg Administration:PO, approximately 2 h prior to tussive agent exposure Result:Significantly reduced the histamine-induced enhancement in the number of citric acid-induced coughs. Reduced significantly and dose-dependently the ATP-induced enhancement of citric acid-induced coughs.

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Membrane Transporter/Ion Channel

P2X Receptor

P2X Receptor

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1621164-74-6

458.46

C23H24F2N4O4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (218.12 mM; 超声助溶 ) DMSO 中的溶解度 : 100 mg/mL (218.12 mM; ultrasonic and adjust pH to 3 with 1M HCl )

C(C1=C(N=C2N1C=CC(C)=C2)C3=C(F)C=C(C(NC)=O)C=C3F)[C@H]4CN(C(OC)=O)CCO4

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(-20℃)

With Ice Pack

≥ 2 years