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AF-353 hydrochloride

Product Specifications

Target

Others|||P2X Receptor

Related Pathways

Neuroscience|||Membrane transporter/Ion channel|||Others

Bioactivity

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.

Smiles

O(C1=C(C(C)C)C=C(OC)C(I)=C1)C=2C(N)=NC(N)=NC2.Cl

Molecular Formula

C14H17IN4O2?HCl

Molecular Weight

436.68

Shipping Conditions

Cool pack

Storage Temperature

-20°C

Product Datasheet

https://www.targetmol.com/attachment/DataSheet/187269966754480237/T85192

CAS Number

927887-18-1

Available Sizes

Curated Selection

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