P2X receptor Selective Inhibitors | Antagonists

Catalog No.	Product Name	Information	Selective / Pan	IC50 / Ki
S8513	JNJ-47965567	JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, which can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology.	Selective	human P2X7, pKi: 7.9; rat P2X7, pKi: 8.7
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	hP2X3, pIC50: 8.06; rP2X3, pIC50: 8.05; hP2X2/3, pIC50: 7.41
S8519	A-317491	A-317491 is a novel potent and selective non-nucleotide antagonist of P2X₃ and P2X_2/3 receptors with Ki values of 22 nM and 9 nM for human P2X₃ and P2X_2/3 receptors.	Selective	Human P2X3, Ki: 22 nM; Rat P2X3, Ki: 22 nM; Rat P2X2/3, Ki: 92 nM; Human P2X2/3, Ki: 9 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
S3217	Brilliant Blue G	Brilliant Blue G (BBG) is a dye which is commonly used in laboratories to stain or quantify proteins.Brilliant Blue G 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.	Selective	rat P2X7, IC50: 10.1 nM; human P2X7, IC50: 265 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 is a potent, and selective P2X7 receptor antagonist with pIC50 of 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 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
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
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
S0053	CAY10593 (VU0155069)	CAY10593 (VU0155069) is a selective phospholipase D1 (PLD1) antagonist that impairs human P2X7 acivation.	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