2. Metabolic Enzyme/Protease
  3. Glucokinase
  4. AMG-1694

AMG-1694 是一种有效的葡萄糖激酶-葡萄糖激酶调节蛋白 (GK-GKRP) 破坏剂，AMG-1694 促进 GK-GKRP 复合物的解离，IC50 为 7 nM，间接增加 GK 酶活性。AMG-1694 有效地逆转 GKRP 对 GK 活性的抑制作用，并促进 GK 易位。AMG-1694 可在几种啮齿动物的糖尿病模型中使血糖水平正常化，并且只能降低糖尿病患者血糖而非血糖正常的动物。

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AMG-1694

AMG-1694 Chemical Structure

CAS No. : 1361217-07-3

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1 mg ￥2620
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AMG-1694 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

AMG-1694 is a potent glucokinase-glucokinase regulatory protein (GK-GKRP) disruptors and promotes the dissociation of the GK-GKRP complex with an IC50 of 7 nM, indirectly increasing GK enzymatic activity. AMG-1694 potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation. AMG-1694 normalizes blood glucose levels in several rodent models of diabetes and lowes blood glucose restricted to diabetic and not normoglycaemic animals[1].

IC50 & Target

IC50: 7 nM (GK-GKRP)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Hepatocyte EC50
0.082 μM
Compound: 25, AMG-1694
Inhibition of GKRP-GK interaction in rat primary hepatocytes assessed as translocation of GK from nucleus to cytoplasm preincubated for 20 mins followed by glucose addition measured after 40 mins by fluorescence assay
Inhibition of GKRP-GK interaction in rat primary hepatocytes assessed as translocation of GK from nucleus to cytoplasm preincubated for 20 mins followed by glucose addition measured after 40 mins by fluorescence assay
[PMID: 24405172]
Hepatocyte EC50
1.79 μM
Compound: 1, AMG-1694
Induction of GK translocation from nucleus to cytoplasm of mouse hepatocytes preincubated for 20 mins followed by glucose challenge measured after 40 mins by Hoechst 33342 staining-based assay
Induction of GK translocation from nucleus to cytoplasm of mouse hepatocytes preincubated for 20 mins followed by glucose challenge measured after 40 mins by Hoechst 33342 staining-based assay
[PMID: 24405213]
体外研究
(In Vitro)

AMG-1694 is highly effective in restoring the enzymatic activity of GK with an EC50 of 0.020 μM in the presence of GKRP[1].

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

AMG-1694 相关抗体:
分子量

533.63

Formula

C23H30F3N3O4S2
CAS 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

AMG-1694 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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:

AMG-16941361217-07-3AMG1694AMG 1694GlucokinaseHexokinase IVHexokinase DInhibitorinhibitorinhibit

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产品名称：
AMG-1694
目录号：
HY-12614
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