| Identification | Back Directory | [Name]
camlipixant | [CAS]
1621164-74-6 | [Synonyms]
camlipixant
(S)-Methyl-2-((2-(2,6-difluoro-4-(methylcarbamoyl)phenyl)-7-methylimidazo[1,2-a]pyridin-3-yl)methyl)morpholine-4-carboxylate
4-Morpholinecarboxylic acid, 2-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (2S)- | [Molecular Formula]
C23H24F2N4O4 | [MOL File]
1621164-74-6.mol | [Molecular Weight]
458.46 |
| Chemical Properties | Back Directory | [form ]
Solid | [color ]
White to off-white | [InChIKey]
SEHLMRJSQFAPCJ-HNNXBMFYSA-N | [SMILES]
N1(C(OC)=O)CCO[C@@H](CC2N3C(=NC=2C2=C(F)C=C(C(NC)=O)C=C2F)C=C(C)C=C3)C1 |
| Hazard Information | Back Directory | [Chemical Properties]
Camlipixant is a purinoreceptor antagonist. | [Uses]
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]. | [Biological Activity]
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.
| [in vivo]
Camlipixant (BLU-5937; 3-30 mg/kg; oral) reduces histamine- and ATP- induced cough hypersensitivity in guinea pigs[1].
Camlipixant (BLU-5937; 10-20 mg/kg; i.p.) does not alter taste perception as compared to control animals[1].
Camlipixant (BLU-5937) exhibits excellent drug-like characteristics, including good oral bioavailability, low predicted clearance in human, no blood-brain barrier permeability and high safety margin versus human predicted efficacious exposure[1]. | Animal Model: | Male Dunkin Hartley guinea pigs[1] | | Dosage: | 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. |
| [References]
[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. DOI:10.1016/j.pupt.2019.03.007 |
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ChemCell Biomedicine Co.,Ltd.
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www.chemicalbook.com/ShowSupplierProductsList15061/0_EN.htm |
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