1. GPCR/G Protein
  2. Apelin Receptor (APJ)
  3. APJ receptor agonist 1

APJ receptor agonist 1 是一种联苯酸衍生物,是一种有效的 APJ 受体 (APJ-R) 激动剂 (EC50s 为 0.093 和 0.12 nM,分别适用于人和大鼠的 APJ-R)。APJ receptor agonist 1 在体外表现出对 apelin-13 的效力,apelin-13 是 APJ 受体的内源性肽配体。APJ receptor agonist 1 具有研究心力衰竭的潜力。

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APJ receptor agonist 1 Chemical Structure

APJ receptor agonist 1 Chemical Structure

CAS No. : 2287153-38-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

APJ receptor agonist 1, a biphenyl acid derivative, is a potent APJ receptor (APJ-R) agonist (EC50s 0.093 and 0.12 nM for human and rat APJ-R, respectively). APJ receptor agonist 1 displays in vitro potency to apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 has the potential for the research of heart failure[1].

体外研究
(In Vitro)

The S-atropisomer APJ receptor agonist 1 (compound 15a) is 200-fold more potent than the corresponding R-atropisomer.[1].

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

体内研究
(In Vivo)

APJ receptor agonist 1 (10-100 μg/min/kg; intravenous infusion) induces a 10% increase in CO with minimal impact on blood pressure (<5% transient blood pressure drop)[1].

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

Animal Model: Isoflurane-anesthetized male Sprague Dawley rats[1]
Dosage: 10, 100, 1000 μg/kg/min
Administration: IV; infused into the jugular vein for 15 min
Result: Showed a dose-dependent improvement in the cardiac output in male Sprague Dawley rats with no significant changes in either mean arterial blood pressure or heart rate.
分子量

524.01

Formula

C31H26ClN3O3

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

APJ receptor agonist 1 相关分类

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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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APJ receptor agonist 1
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HY-133036
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