Camlipixant, also known as BLU-5937, is a potent, selective and non-competitive P2X3 homotrimeric receptor antagonist. The IC50 of BLU-5937 for hP2X3 homotrimeric and hP2X2/3 heterotrimeric receptors was established at 25 nM and >24 μM, respectively. Furthermore, BLU-5937 (500 nM) was 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. In a guinea pig cough model, BLU-5937 (0.3, 3 and 30 mg/kg, oral) significantly reduced, in a dose-dependent fashion, the histamine-induced enhancement in the number of citric acid-induced coughs. BLU-5937 (3 and 30 mg/kg, oral) was also shown to reduce significantly and dose-dependently the ATP-induced enhancement of citric acid-induced coughs in the guinea pig.
MedKoo Cat#: 121067
Name: Camlipixant
CAS#: 1621164-74-6
Chemical Formula: C23H24F2N4O4
Exact Mass: 458.1766
Molecular Weight: 458.47
Elemental Analysis: C, 60.26; H, 5.28; F, 8.29; N, 12.22; O, 13.96
The following data is based on the product molecular weight 458.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
