P2X2/3-antagonist-1

P2X2/3-antagonist-1 potently (compound 30) inhibits human P2X2/3 receptor activity in CHO cells coexpressing human P2X2 and P2X3 with a pIC₅₀ of 8.1^[1].
P2X2/3-antagonist-1 (1 nM-1 μM; 30 nM) acts as an allosteric antagonist of human P2X2/3 receptors in CHO cells coexpressing human P2X2 and P2X3, with a pK_B of 8.7, and shares a binding site with AF-353 (1)^[1].
P2X2/3-antagonist-1 exhibits moderate-high permeability in MDCK wild-type cells, with a P_app value of 6.2 × 10^-6 cm/s^[1].
P2X2/3-antagonist-1 has a kinetic solubility of 106 μM in PBS at pH 7.4^[1].
P2X2/3-antagonist-1 has a log D value of 3.2 in 1-octanol/PBS at pH 7.4^[1].
P2X2/3-antagonist-1 (10 μM) has a low risk of cytochrome P450-related interactions, with weak inhibition of CYP2C8 and CYP2C9 at 10 μM and no time-dependent inhibition of CYP3A4^[1].
P2X2/3-antagonist-1 (30 μM) exhibits minimal off-target activity in a 47-target safety panel, with only 54% inhibition of CCK1 at 30 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.