- P2X receptor
- P2Y receptor
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|
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|
A-317491是一种新型的、有效的、选择性的P2X3和P2X2/3受体的非核苷类拮抗剂，对人源P2X3和P2X2/3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|
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|
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|
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|
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|
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|
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.
|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)
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.
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