G protein-coupled receptors (GPCRs) known as P2Y receptors are activated by the extracellular nucleotides ATP, UTP, and UDP. Mammalian P2Y receptors come in eight different subtypes: P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, P2Y13, and P2Y14. The P2Y receptors play significant roles in physiology and pathophysiology, including inflammatory reactions and neuropathic pain, and are expressed in a variety of cell types.
The P2Y family can be further divided into two subfamilies: P2Y12, P2Y13, and P2Y14Rs ("P2Y12-like"), which inhibit adenylate cyclase through Gi protein, and P2Y1, P2Y2, P2Y4, P2Y6, and P2Y11Rs ("P2Y1-like"), which stimulate phospholipase C (PLC) through Gq protein. Other effector pathways have also been identified, such as the coupling of the P2Y11R to Gs and Gq in some cells to stimulate the production of cyclic AMP.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V74436 | 2-Methylthio-AMP (2-MeSAMP; 2-Methylthioadenosine 5′-monophosphate; 2-Methylthioadenosine 5′-phosphate) | 22140-20-1 | 2-Methylthio-AMP (2-MeSAMP) is a selective and direct P2Y12 antagonist. |
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V74442 | 2-Methylthio-AMP diTEA (2-MeSAMP diTEA; 2-Methylthioadenosine 5′-monophosphate diTEA; 2-Methylthioadenosine 5′-phosphate diTEA) | 1227193-98-7 | 2-Methylthio-AMP (2-MeSAMP) diTEA is a selective and direct P2Y12 antagonist. |
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V3528 | 2MeSADP | 475193-31-8 | 2MeSADP is a novel and potent purinergic agonist which acts by displaying selectivity for P2Y1, P2Y12 and P2Y13 receptors and inhibiting cAMP accumulation. |
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V74435 | 3-O-Methylquercetin tetraacetate (Quercetin 3-O-methyl ether peracetate) | 1486-69-7 | 3-O-Methylquercetin tetraacetate is an antiplatelet agent. |
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V74448 | 4-Thiouridine 5′-triphosphate tetralithium (4-Thio-UTP tetralithium) | 20188-72-1 | 4-Thouridine 5′-triphosphate (4-Thio-UTP) tetralithium is a potent agonist of P2Y2 and P2Y4 with EC50s of 35 and 350 nM for hP2Y2 and hP2Y4, respectively. |
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V77629 | 4-Thouridine 5′-triphosphate tetrasodium (4-Thio-UTP tetrasodium) | 4-Thouridine 5′-triphosphate (4-Thio-UTP) tetrasodium is a potent agonist of P2Y2 and P2Y4 with EC50s of 35 and 350 nM for hP2Y2 and hP2Y4, respectively. | |
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V51183 | Adenosine 2',5'-diphosphate sodium | 154146-84-6 | Adenosine 2',5'-sodium diphosphate is a competitive P2Y1 antagonist. |
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V74434 | ATP-γ-S tetrasodium | 88453-52-5 | ATP-γ-S tetrasodium is an ATP analog and a P2Y11 receptor agonist. |
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V4242 | AZD-1283 | 919351-41-0 | AZD1283 is a novel, potent and selective antagonist of the P2Y12 receptor with EC50 of 3.0 ug/kg/min, TI >10 and with binding IC50 of 11 nM. |
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V73575 | Blue FPG-A trisodium | 78617-94-4 | Blue FPG-A trisodium is a selective P2X1 receptor and P2Y1 receptor antagonist (inhibitor) with IC50s of 35.5 μM and 2.6 μM respectively. |
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V3526 | BPTU | 870544-59-5 | BPTU (BMS-646786),a non-nucleotide structure, is anew P2Y1 antagonist which has recently been described using X-ray crystallography as the first allosteric G-protein-coupled receptor antagonist located entirely outside of the helical bundle. |
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V23187 | Cangrelor sodium | 163706-36-3 | Cangrelor sodium (ARC69931MX; AR-C69931; Kengreal, CANREAL; Kengrexal), the tetra-sodium salt of cangrelor which is an ATP analog, is a reversible, selective and direct-acting P2Y12 inhibitor approved in June 2015 as an antiplatelet drug for intravenous application. |
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V74432 | Clopidogrel (Clopidogrel; Clopidogrelum) | 113665-84-2 | Clopidogrel is an orally bioactive platelet inhibitor targeting the P2Y12 receptor. |
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V3330 | Clopidogrel thiolactone | 1147350-75-1 | Clopidogrel thiolactone (also known as 2-Oxoclopidogrel) is a metabolite of Clopidogrel which is a P2Y12 receptor inhibitor. |
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V5253 | Diquafosol Tetrasodium (INS365) | 211427-08-6 | Diquafosol tetrasodium (Diquas; INS-365) is a novel and potent P2Y2 purinoceptor agonist that stimulates fluid and mucin secretion on the ocular surface, and is used as a topical treatment of dry eye disease. |
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V74441 | MRS2179 tetrasodium | 1454889-37-2 | MRS2179 tetrasodium is a competitive P2Y1 receptor antagonist (inhibitor) with a Kb value of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptors. |
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V76746 | MRS2179 tetrasodium hydrate | MRS2179 tetrasodium hydrate is a competitive P2Y1 receptor antagonist (inhibitor) with a Kb value of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptors. | |
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V74440 | MRS2279 diammonium | 2387505-47-5 | MRS2279 diammonium is a selective, high-affinity P2Y1 receptor antagonist (inhibitor) with a Ki of 2.5 nM and IC50 of 51.6 nM. |
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V80553 | MRS2365 trisodium | MRS2365 trisodium is a potent and specific P2Y1 receptor (EC50=0.4 nM)/[35S]GTPγS binding/β-arrestin 2 recruiting agonist. | |
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V74443 | MRS2768 tetrasodium salt | 2567869-47-8 | MRS2768 tetrasodium salt is a moderately potent and specific P2Y2 receptor agonist. |
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