1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase
  3. DPP-4-IN-17

DPP-4-IN-17 是一种口服活性的选择性二肽基肽酶-4 (DPP-4) 抑制剂,其 IC50 值为 0.12 nM。DPP-4-IN-17 增加酶的 Km 值 (75.73 μM 对比底物单独的 27.18 μM) 并降低催化效率。DPP-4-IN-17 在 Streptozotocin (STZ) (HY-13753)/Nicotinamide (NA) (HY-B0150) 诱导的糖尿病大鼠中降低血糖水平并逆转体重减轻。DPP-4-IN-17 可用于研究 2 型糖尿病 (T2DM)。

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DPP-4-IN-17

DPP-4-IN-17 Chemical Structure

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查看 Dipeptidyl Peptidase 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DPP-4-IN-17 is an orally active and selective dipeptidyl peptidase-4 (DPP-4) inhibitor with an IC50 value of 0.12 nM. DPP-4-IN-17 increases the enzyme's Km value (75.73 μM vs. 27.18 μM of substrate alone) and reduces catalytic efficiency. DPP-4-IN-17 reduces blood glucose levels and reverses weight loss in Streptozotocin (STZ) (HY-13753)/Nicotinamide (NA) (HY-B0150)-induced diabetic rats. DPP-4-IN-17 can be used for the study of type 2 diabetes mellitus (T2DM)[1].

IC50 & Target[1]

DPP-4

0.12 nM (IC50)

体外研究
(In Vitro)

DPP-4-IN-17 (Compound 8) 作为一种竞争性 DPP-4 抑制剂,将 Km 值从 27.18 μM 增加到 75.73 μM,并降低催化效率[1]

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

体内研究
(In Vivo)

DPP-4-IN-17 (Compound 8) (10-40 mg/kg,口服给药,每日一次,持续 21 天) 在 Streptozotocin (STZ) (HY-13753)/Nicotinamide (NA) (HY-B0150) 诱导的糖尿病 Wistar 大鼠中显著降低血糖水平并逆转体重减轻[1]

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

Animal Model: Wistar rats (6-8 weeks, 200-250 g) were fasted overnight (12 h), ip injected with 110 mg/kg nicotinamide (NA); 15 min later, ip injected with 50 mg/kg streptozotocin[1]
Dosage: 10, 20, 40 mg/kg
Administration: p.o., once daily, 21 days
Result: Reduced blood glucose to normal.
Reversed weight loss.
Normalized serum lipids, liver enzymes and renal parameters.
Repaired kidney (glomerulosclerosis reversed, tubule integrity restored) and pancreas (islet β-cells increased, acinar cells/ducts intact).
分子量

651.79

Formula

C32H53N5O9

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
DPP-4-IN-17
目录号:
HY-175590
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