1. GPCR/G Protein Neuronal Signaling
  2. GPR119
  3. GPR119 agonist 4

GPR119 agonist 4 是一种口服有效的 GPR119 激动剂,其 EC50 值为 42 nM。GPR119 agonist 4 可降低口服葡萄糖耐量试验中的血糖曲线下面积。GPR119 agonist 4 在肝微粒体中表现出改善的清除率。GPR119 agonist 4 可用于 2 型糖尿病的研究。

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GPR119 agonist 4

GPR119 agonist 4 Chemical Structure

CAS No. : 1353004-92-8

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  • 生物活性

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生物活性

GPR119 agonist 4 is a GPR119 agonist and oral glucose-lowering agent with a human GPR119 EC50 of 42 nM.GPR119 agonist 4 activates GPR119.GPR119 agonist 4 reduces blood glucose area under the curve in an oral glucose tolerance test.GPR119 agonist 4 exhibits improved clearance in liver microsomes.GPR119 agonist 4 can be used for the research of type 2 diabetes mellitus[1].

体外研究
(In Vitro)

GPR119 agonist 4 (Compound 26) 具有提升的代谢稳定性,在人肝微粒体中的清除率为 113 μL/min/mg/protein,在小鼠肝微粒体中的清除率为 108 μL/min/mg/protein[1]

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

药代动力学
(Parmacokinetics)
Species Dose Route CLplasma Vss T1/2 Cmax AUC Bioavailability
Mice[1] 0.5 mg/kg i.v. 6.5 mL/min/kg 2.3 L/kg 5.1 h / / /
Mice[1] 10 mg/kg p.o. / / / 2015 ng/mL 9386 ng·h/mL 37 %
体内研究
(In Vivo)

GPR119 agonist 4 (Compound 26) (10 mg/kg;口服;单剂量) 在 C57BL/6N 小鼠的口服葡萄糖耐量试验中,于 10 mg/kg 剂量下可使血糖 AUC0-t 降低 33%[1]

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

Animal Model: C57BL/6N mice[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose
Result: Induced a 33% reduction in blood glucose area under the curve (AUC) during the oral glucose tolerance test.
分子量

511.00

Formula

C24H23ClN6O3S

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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GPR119 agonist 4
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HY-182454
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