2. GPCR/G Protein
  3. Apelin Receptor (APJ)
  4. APJ receptor agonist 4

APJ receptor agonist 4 是一种有效的、具有口服活性的 apelin receptor (APJ) 激动剂，EC50 和 Ki 为 0.06 nM 和 0.07 nM。APJ receptor agonist 4 在啮齿动物心力衰竭模型中表现出优异的药代动力学特征。APJ receptor agonist 4 在临床前毒理学研究中也显示出可接受的安全性。APJ receptor agonist 4 可改善心功能，并可用于研究心力衰竭疾病。

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APJ receptor agonist 4 Chemical Structure

APJ receptor agonist 4 Chemical Structure

CAS No. : 2762567-70-2

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APJ receptor agonist 4 相关抗体

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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 4 is a potent and orally active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease[1].

IC50 & Target

apelin receptor[1]
体内研究
(In Vivo)

Assessment of Pharmacokinetics (PK) profile of APJ receptor agonist 4 (compound 21) in mouse[1].

species rat monkey dogmax (ng/mL)
dose (mg/kg) 1 (i.v. and p.o.) 1 (i.v.) and 3 (p.o.) 1 (i.v. and p.o.)
vehiclea F G G
CI (mL/min/kg) 4.6 10.6 2.4
VSS (L/kg) 1.6 0.2 0.2
T1/2 (h) 4.0 1.3 2.5
Cmax (μM•h) 2.2 1.4 6.5
AUC0-24 (μM•h) 3.7 2.5 14.2
F (%) 54 27 76

a: Vehicle F: 5/5/90 v/v/v DMAC/Cremophor EL/sodium carbonate buffer, pH 9 and vehicle G: 10/40/50 v/v/v ethanol/PEG400/sodium carbonate buffer, pH 9.

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

551.01

Formula

C28H28ClFN6O3
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 4 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.

Keywords:

APJ receptor agonist 42762567-70-2APJ receptor agonist4APJ receptor agonist-4Apelin Receptor (APJ)apelin receptorAPJheart failureselectiveoralInhibitorinhibitorinhibit

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