CAS 927887-18-1

5-[5-iodo-4-methoxy-2-(1-methylethyl)phenoxy]-2,4-pyrimidinediamine hydrochloride

CAS: 927887-18-1

Formula: C₁₄H₁₈ClIN₄O₂

Peso molecolare: 436.6758

Ref: IN-DA0035VC

AF-353 hydrochloride

CAS: 927887-18-1

This novel compound is an orally bioavailable antagonist of P2X3/P2X2/3 receptors, exhibiting potent activity with a pIC50 of 8 in both human and rat, and a pIC50 of 7.3 specifically for the human P2X2/3 receptor. It demonstrates high brain penetration, evidenced by a brain to plasma ratio of 6, and effectively blocks agonist-evoked intracellular Ca2+ flux and inward currents within the nanomolar range (10 nM to 1 µM) in cell lines that express human P2X3 and P2X2/3 receptors recombinantly. The compound also shows favorable pharmacokinetic properties, with a half-life (t1/2) of 1.63 hours and a time to reach maximum concentration (Tmax) of 30 minutes.

Formula: C₁₄H₁₇IN₄O₂HCl

Colore e forma: Solid

Peso molecolare: 436.68

Ref: TM-T85192