P2X receptor Selective Inhibitors | Antagonists

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S0053 CAY10593 (VU0155069)

CAY10593 (VU0155069) is a selective phospholipase D1 (PLD1) antagonist that impairs human P2X7 acivation.

Selective
S0405 AF-353

AF-353 (Ro-4) is a potent, selective and orally bioavailable antagonist of P2X3 receptor and P2X2/3 receptor with pIC50 of 8.06, 8.05 and 7.41 for human P2X3, rat P2X3 and human P2X2/3, respectively.

Selective hP2X2/3, pIC50: 7.41; rP2X3, pIC50: 8.05; hP2X3, pIC50: 8.06
S0758 BX430

BX430 is a potent and selective noncompetitive allosteric antagonist of human P2X4 receptor channels with IC50 of 0.54 μM. BX430 is a potent antagonist of zebrafish P2X4 but has no effect on rat and mouse P2X4 orthologs. BX430 is used for chronic pain and cardiovascular disease.

Selective hP2X4, IC50: 0.54 μM
S0826 A-740003

A-740003 is a potent, selective and competitive antagonist of P2X7 receptor with IC50 of 18 nM and 40 nM for rat and human P2X7 receptors, respectively. A-740003 potently blocks agonist-evoked IL-1β release and pore formation with IC50 of 156 nM and 92 nM in differentiated human THP-1 cells.

Selective human P2X7 receptor, IC50: 40 nM; rat P2X7 receptor, IC50: 18 nM
S3217 Brilliant Blue G

Brilliant Blue G (BBG) is a potent non-competitive antagonist of P2X7 receptor with IC50 of 10.1 nM and 265 nM for rat P2X7 and human P2X7, respectively. Brilliant Blue G is a dye which is commonly used in laboratories to stain or quantify proteins.

Selective human P2X7, IC50: 265 nM; rat P2X7, IC50: 10.1 nM
S3293 Gardenoside

Gardenoside is a natural compound extracted from Gardenia fruits, with hepatoprotective properties. Gardenoside inhibits TNF-α, IL-1β, IL-6 and NFκB activation. Gardenoside also has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. Gardenoside suppresses the pain in rats model of chronic constriction injury by regulating the P2X3 and P2X7 receptors.

Pan
S3766 Tanshinone IIA sulfonate sodium

Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE)

Selective
S6664 Gefapixant

Gefapixant (AF-219, MK-7264, R1646, RG-1646, RO 4926219) is an orally active small molecule antagonist of human P2X3 receptor with IC50 of about 30 nM, 100–250 nM for recombinant hP2X3 homotrimers and hP2X2/3 heterotrimeric receptors, respectively. Gefapixant has shown promise for the treatment of refractory and unexplained chronic cough.

Selective hP2X2/3, IC50: 100-250 nM; hP2X3, IC50: 30 nM
S7705 A-438079 HCl

A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.

Selective P2X7, pIC50: 6.9
S8519 A-317491

A-317491 is a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors with Ki values of 22 nM and 9 nM for human P2X3 and P2X2/3 receptors.

Selective Human P2X2/3, Ki: 9 nM; Rat P2X2/3, Ki: 92 nM; Rat P2X3, Ki: 22 nM; Human P2X3, Ki: 22 nM
S8725 A-804598

A-804598 is a selective P2X7R antagonist with high affinity at rat (IC50 = 10 nM), mouse (IC50 = 9 nM) and human (IC50 = 11 nM) P2X7 receptors.

Selective rat P2X7R, IC50: 10 nM; rat P2X7R, IC50: 9 nM; human P2X7R, IC50: 11 nM
S9498 5-BDBD

5-BDBD is a potent P2X4R selective antagonist with an IC50 of 0.75 μM when applied for 2 min prior and during ATP stimulation.

Selective