P2X receptor 选择性抑制剂 | 拮抗剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S0405 AF-353

AF-353 (Ro-4) is a potent, selective and orally bioavailable antagonist of P2X3/P2X2/3 receptor with pIC50 of 8.0, 8.0 and 7.3 for human P2X3, rat P2X3 and human P2X2/3, respectively.

Selective hP2X2/3, pIC50: 7.41; hP2X3, pIC50: 8.06; rP2X3, pIC50: 8.05
S8519 A-317491

A-317491是一种新型的、有效的、选择性的P2X3P2X2/3受体的非核苷类拮抗剂,对人源P2X3P2X2/3的Ki值分别为22 nM和9 nM。

Selective Rat P2X2/3, Ki: 92 nM; Human P2X2/3, Ki: 9 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 human P2X7R, IC50: 11 nM; rat P2X7R, IC50: 9 nM; rat P2X7R, IC50: 10 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
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 rat P2X7 receptor, IC50: 18 nM; human P2X7 receptor, IC50: 40 nM
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 hP2X3, IC50: 30 nM; hP2X2/3, IC50: 100-250 nM
S7705 A-438079 HCl

A-438079 HCl 是一种有效的选择性 P2X7 receptor 拮抗剂,pIC50 为 6.9。

Selective P2X7, pIC50: 6.9
S0758 BX430

BX430 is a potent and selective noncompetitive allosteric antagonist of human P2X4 receptor channels with IC50 of 0.54 μM. BX430 has species specificity and is used for chronic pain and cardiovascular disease.

Selective hP2X4, IC50: 0.54 μM
S0053 CAY10593 (VU0155069)

CAY10593 (VU0155069) is a selective phospholipase D1 (PLD1) inhibitor with IC50 of 46 nM in vitro. CAY10593 (VU0155069) strongly inhibits the invasive migration of several cancer cell lines in transwell assays.

Selective
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
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