MRS2279 是一种选择性、高亲和力的 P2Y1 受体拮抗剂，Ki 为 2.5 nM，IC50 为 51.6 nM。MRS2279 竞争性抑制 ADP 促进的血小板聚集，并具有亲和性 (pKB=8.05)
| 生物活性 |
MRS2279 is a selective and high affinity P2Y1 receptor antagonist, with a Ki of 2.5 nM and an IC50 of 51.6 nM. MRS2279 competitively inhibits ADP-promoted platelet aggregation with an apparent affnity (pKB=8.05). |
|---|---|
| 体外研究 |
MRS2279 antagonized 2MeSADP-stimulated inositol phosphate formation in turkey erythrocyte membranes with competitive kinetics (pKB=7.75). High affinity competitive antagonism by MRS2279 was also observed at the human P2Y1 receptor (pKB=8.10) stably expressed in 1321N1 human astrocytoma cells. Antagonism was specific for the P2Y1 receptor since MRS2279 had no effect on activation of the human P2Y2, P2Y4, P2Y6, or P2Y11 receptors by their cognate agonists. MRS2279 also did not block the capacity of ADP to act through the Gi/adenylyl cyclase linked P2Y receptor of platelets to inhibit cyclic AMP accumulation. |
| 分子式 |
C13H18N5O8P2Cl
|
| 分子量 |
469.71
|
| CAS号 |
367909-40-8
|
| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
客服小K 
客服小K
Data Sheet
