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BLU-5937

Chemical Structure : BLU-5937

CAS No.: 1621164-74-6

BLU-5937 (Camlipixant, BLU5937)

Catalog No.: PC-20741Not For Human Use, Lab Use Only.

BLU-5937 (Camlipixant, BLU5937) is a potent, selective and non-competitive P2X3 homotrimeric receptor antagonist with IC50 of 25 and 92 nM for human and rat P2X3 receptors, repsectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

BLU-5937 (Camlipixant, BLU5937) is a potent, selective and non-competitive P2X3 homotrimeric receptor antagonist with IC50 of 25 and 92 nM for human and rat P2X3 receptors, repsectively.
BLU-5937 displays 1500-fold selectivity for human P2X3 over human P2X2/3.
BLU-5937 (500 nM) effectively inhibits P2X3-mediated sensitization of rat DRG neurons, blocks ATP-mediated neuron sensitization by inhibiting P2X3 homotrimeric receptors.
BLU-5937 (0.3-30 mg/kg, orally) reduces histamine- and ATP- induced cough hypersensitivity in guinea pigs.
BLU-5937 significantly reduced ATP- and histamineinduced enhancement in number of citric acid-induced coughs in the guinea pig.

Physicochemical Properties

M.Wt 458.47
Formula C23H24F2N4O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

O=C(N1C[C@H](CC2=C(C3=C(F)C=C(C(NC)=O)C=C3F)N=C4C=C(C)C=CN42)OCC1)OC

References

1. Garceau D, et al. Pulm Pharmacol Ther. 2019 Jun;56:56-62.

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