1. GPCR/G Protein
  2. P2Y Receptor
  3. MRS2279

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)

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 MRS2279 diammonium 通常具有更好的水溶性和稳定性。

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MRS2279 Chemical Structure

MRS2279 Chemical Structure

CAS No. : 367909-40-8

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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)[1][2][3].

IC50 & Target

P2Y1 Receptor

51.6 nM (IC50)

体外研究
(In Vitro)

MRS2279 antagonizes 2-MeSADP-stimulated inositol phosphate formation in turkey erythrocyte membranes with a pKb value of 7.75[2].
MRS2279 shows high affinity competitive antagonism to human P2Y1 receptor with a pKb value of 8.10 in 1321N1 human astrocytoma cells[2].
MRS2279 shows specific effect for the P2Y1 receptor, but shows no effect on activation of the human P2Y2, P2Y4, P2Y6, or P2Y11 receptors by their cognate agonists[2].
MRS2279 shows no ability to block the capacity of ADP to act through the Gi/adenylyl cyclase linked P2Y receptor of platelets to inhibit cyclic AMP accumulation[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

MRS2279 (2 μL, 1 nM; intracerebroventricular injection; 30 min prior to mechanical ventilation) reduces mouse brain injury induced by mechanical ventilation in high-pressure ventilation mice[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

469.71

Formula

C13H18ClN5O8P2

CAS 号
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.

纯度 & 产品资料
参考文献

MRS2279 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
MRS2279
目录号:
HY-108657
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