P2 Receptor Agonists
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
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| S7705 | A-438079 Hydrochloride | A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9. |
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| S4079 | Ticagrelor | Ticagrelor (AZD6140, AR-C 126532XX) is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM. |
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| 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. |
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| S1258 | Prasugrel | Prasugrel (Effient, Efient, Prasita, CS-747, LY640315, PCR 4099) is a thienopyridine ADP receptor (P2Y12) antagonist, used for the reduction of thrombotic cardiovascular events. |
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| 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. This compound potently blocks agonist-evoked IL-1β release and pore formation with IC50 of 156 nM and 92 nM in differentiated human THP-1 cells. |
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| S3217 | Brilliant Blue G | Brilliant Blue G (BBG) is a dye which is commonly used in laboratories to stain or quantify proteins. This compound 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. |
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| 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. |
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| 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. This compound has shown promise for the treatment of refractory and unexplained chronic cough. |
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| 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. |
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| 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. | ||
| S0758 | BX430 | BX430 is a potent and selective noncompetitive allosteric antagonist of human P2X4 receptor channels with IC50 of 0.54 μM. This compound is a potent antagonist of zebrafish P2X4 but has no effect on rat and mouse P2X4 orthologs. It is used for chronic pain and cardiovascular disease. | ||
| E0357 | Eliapixant |
Eliapixant (BAY1817080) is a highly potent and selective P2X3 receptor antagonist with a mean IC50 of 8 nM. |
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| 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. | ||
| S3520 | AZ10606120 dihydrochloride | AZ10606120 dihydrochloride (2HCl) is a potent and selective antagonist for P2X7 receptor (P2X7R) with IC50 of ~10 nM. This compound exhibits anti-depressant effects and reduces tumour growth. This product is not soluble in PBS solution. Please do not dissolve it in PBS for administration. | ||
| S6087 | Indophagolin | Indophagolin, a potent indoline-containing autophagy inhibitor with IC50 of 140 nM, antagonises the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively, also has a strong antagonistic effect on serotonin receptor 5-HT6 with IC50 of 1.0 μM. | ||
| S5057 | Minodronic acid | Minodronic acid (YM529, ONO-5920) is a third-generation nitrogen-containing bisphosphonate that is used for the treatment of osteoporosis. This compound is an aminobisphosphonate that is a selective antagonist of purinergic P2X2/3 receptors involved in pain. |
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