4-Morpholinecarboxylic acid, 2-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (2S)-
- Product Name
- 4-Morpholinecarboxylic acid, 2-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (2S)-
- CAS No.
- 1621164-74-6
- Chemical Name
- 4-Morpholinecarboxylic acid, 2-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (2S)-
- Synonyms
- camlipixant;Camlipixant(BLU-5937);Camlipixant, 10 mM in DMSO;P2X3 homotrimeric receptor antagonist Camlipixant (BLU-5937);(S)-Methyl-2-((2-(2,6-difluoro-4-(methylcarbamoyl)phenyl)-7-methylimidazo[1,2-a]pyridin-3-yl)methyl)morpholine-4-carboxylate;methyl (2S)-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)-
- CBNumber
- CB98106170
- Molecular Formula
- C23H24F2N4O4
- Formula Weight
- 458.46
- MOL File
- 1621164-74-6.mol
4-Morpholinecarboxylic acid, 2-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (2S)- Property
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P501Dispose of contents/container to..…
4-Morpholinecarboxylic acid, 2-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (2S)- Chemical Properties,Usage,Production
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
4-Morpholinecarboxylic acid, 2-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (2S)- Preparation Products And Raw materials
Raw materials
Preparation Products
4-Morpholinecarboxylic acid, 2-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (2S)- Suppliers
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