2. 疾病领域
  3. 代谢或内分泌疾病
  4. (rel)-AM-6226

(rel)-AM-6226 是 AM-6226 (HY-120493A) 的相对立体异构体。AM-6226 是一种强效且具有口服活性的 G 蛋白偶联受体 40 (GPR40) 完全激动剂，其 EC50 值为 0.12 μM。AM-6226 能够激活胰腺 β 细胞和肠内分泌 L 细胞上的 GPR40 受体，以葡萄糖依赖的方式促进胰岛素分泌，还能增加肠促胰岛素激素 (GLP-1, GIP) 的释放，从而避免低血糖风险。AM-6226 可用于代谢性疾病的研究，如糖尿病。

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(rel)-AM-6226

(rel)-AM-6226 Chemical Structure

CAS No. : 1142222-28-3

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(rel)-AM-6226 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

(rel)-AM-6226 is the relative stereoisomer of AM-6226 (HY-120493A). AM-6226 is a potent, orally active full agonist of G protein-coupled receptor 40 (GPR40) with an EC50 value of 0.12 μM. AM-6226 activates GPR40 receptors on pancreatic β-cells and enteroendocrine L-cells, promotes insulin secretion in a glucose-dependent manner, and increases the release of incretin hormones (GLP-1, GIP), thus avoiding the risk of hypoglycemia. AM-6226 can be used in the research of metabolic diseases such as diabetes[1].

体外研究
(In Vitro)

AM-6226 (Compound 14) 在低表达 GPR40 的转染 CHO 细胞中可作为强效 GPR40 完全激动剂，其 EC50 为 0.12 μM，相对于 AM-1638 的效能为 104%[1]。

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

(rel)-AM-6226 相关抗体:
体内研究
(In Vivo)

AM-6226 (0.1-10 mg/kg；灌胃；单剂量) 可在口服葡萄糖耐量试验 (OGTT) 中显著降低前驱糖尿病食蟹猴的血浆葡萄糖水平，10 mg/kg 剂量下血浆葡萄糖 AUC0-t 降低 18%[1]。

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

Animal Model: Cynomolgus monkeys (prediabetic, from high-fat feed colony)[1]
Dosage: 0.1 mg/kg; 1 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Produced significant plasma glucose lowering during the OGTT at 1 mg/kg and 10 mg/kg.
Reduced plasma glucose area under the curve (AUC) by 18% at 10 mg/kg.
分子量

522.62

Formula

C32H36F2O4
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

(rel)-AM-6226 相关分类

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  • 稀释计算器

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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:

(rel)-AM-62261142222-28-3GPR40 ActivatorInhibitorinhibitorinhibit

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产品名称：
(rel)-AM-6226
目录号：
HY-120493
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