| DC40984 |
trans-R-138727MP
|
trans-R-138727MP (Prasugrel metabolite R-138727MP) is the active metabolite derivative of Prasugrel. Prasugrel, a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
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| DC1101 |
Ticagrelor (Brilinta,AZD6140)
|
Ticagrelor is the first reversibly binding oral P2Y12 receptor antagonist, also inhibits CYP2C9 and 4-hydroxylation with IC50 of 10.5 μM and 8.2 μM respectively. |
| DC7203 |
MRS 2578
|
MRS2578 is a potent P2Y6 receptor antagonist with IC50 of 37 nM, exhibits insignificant activity at P2Y1, P2Y2, P2Y4,and P2Y11 receptors. |
| DC73485 |
MRS4853
|
MRS4853 is a selective P2Y6 receptor (P2Y6R) antagonist with IC50 of 0.46 uM (hP2Y6R), displays weak affinity for mP2Y6R (IC50=6.15 uM). |
| DC73484 |
MRS4833
|
MRS4833 is a potent, selective antagonist of Gi protein-coupled P2Y14 receptor (P2Y14R, GPR105) with IC50 of 5.9 nM, Ki of 3.44 nM (human P2Y14R). |
| DC72346 |
MRS2279 diammonium
|
MRS2279 diammonium is a selective and high affinity P2Y1 receptor antagonist, with a Ki value of 2.5 nM and an IC50 value of 51.6 nM. MRS2279 diammonium competitively inhibits ADP-promoted platelet aggregation with an pKb value of 8.05. |
| DC72345 |
PIT
|
PIT (2,2'-Pyridylisatogen tosylate) is a selective and non-competitive antagonist of P2Y1 receptor with an IC50 value of 0.14 μM for human P2Y1 receptor. PIT antagonizes P2Y1 receptor signaling without affecting nucleotide binding. PIT is an irreversible antagonist of responses to ATP at metabotropic purinoceptors (of the P2Y family) in some smooth muscles. PIT can be used for the research of chronic bronchitis and asthma. |
| DC71350 |
PSB 0474
|
PSB 0474 (3-phenacyl-UDP) is a selective and potent P2Y6 receptor agonist with an EC50 of 70 nM. PSB 0474 inhibits cell proliferation, increases NO release in astrocytes and microglia cells. PSB 0474 induces astrocytes apoptosis. |
| DC71349 |
NF340
|
NF340 is a potent and selective P2Y11 receptor antagonist. NF340 inhibits the activity of P2Y11R by completely combining with ATP-binding amino acid residues. NF340 ameliorates inflammation in human fibroblast-like synoviocytes and can be used for rheumatoid arthritis research. |
| DC49652 |
MRS2395
|
MRS2395, an dipivaloyl derivative, is a potent P2Y12 receptor antagonist. MRS2395 inhibits ADP-induced platelet activation with a Ki of 3.6 μM. MRS2395 inhibits cAMP induced by ADP in rat platelets in the presence of PGE1 with an IC50 of 7 µM. MRS2395 enhances platelet dense granule release in response to TRAP-6. |
