1. Membrane Transporter/Ion Channel Cell Cycle/DNA Damage
  2. P2X Receptor Nucleoside Antimetabolite/Analog
  3. MRS2339

MRS2339 是一种核糖修饰的核苷酸,也是核苷酸酶抗性 P2 受体激动剂。MRS2339 可以激活心肌细胞 P2X4R。MRS2339 可通过心肌细胞 P2X 受体诱导离子电流,减小心肌细胞横截面积与心脏重量/体重比,无血管扩张活性,可延长心肌病小鼠寿命。MRS2339 可用于心力衰竭、心肌病的相关研究。

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MRS2339

MRS2339 Chemical Structure

CAS No. : 436847-13-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MRS2339 is a ribose-modified nucleotide and a nucleotidase-resistant P2 receptor agonist. MRS2339 activates P2X4R in cardiomyocytes. MRS2339 induces ionic currents via cardiomyocyte P2X receptors, reduces cardiomyocyte cross-sectional area and heart weight/body weight ratio, lacks vasodilatory activity, and extends the lifespan of mice with cardiomyopathy. MRS2339 can be used in research related to heart failure and cardiomyopathy[1][2].

IC50 & Target[1]

P2X4 Receptor

 

体外研究
(In Vitro)

MRS2339 (10 μM) 可在分离的野生型及 CSQ 小鼠心室心肌细胞中诱导出一种 P2X 样离子电流,该电流的电压依赖性和反转电位与 2-meSATP 完全一致[1]
MRS2339 (10-9-10-5 M) 在离体野生型小鼠胸主动脉环标本中无血管舒张作用[1]

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

体内研究
(In Vivo)

MRS2339 (微型渗透泵;约 6 μl/天;28 天) 可显著延长心力衰竭模型 CSQ 小鼠的中位寿命,减小心肌细胞横截面积,并降低心脏重量与体重的比值[1]

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

Animal Model: calsequestrin (CSQ) transgenic (TG) mice (either sex, ~3 months old)[1]
Dosage: 3 μM
Administration: miniosmotic pump; ~6 μl/day; 28 days
Result: Increased median lifespan to 115 days (log rank test, P = 0.02) compared to vehicle controls.
Reduced cardiac myocyte cross-sectional area to 281 μm2 (n = 6 mice, P < 0.05 vs.
vehicle).
Reduced heart weight-to-body weight ratio to 10.5 mg/gram (n = 9 hearts, P < 0.05 vs.
vehicle).
分子量

391.70

Formula

C12H15ClN5O6P

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
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  • 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:
MRS2339
目录号:
HY-182642
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