2. Metabolic Enzyme/Protease GPCR/G Protein Stem Cell/Wnt TGF-beta/Smad MAPK/ERK Pathway
  3. Dipeptidyl Peptidase GLP Receptor Endogenous Metabolite PKA ERK
  4. Sitagliptin hydrochloride

Sitagliptin hydrochloride  (Synonyms: MK-0431 hydrochloride)

目录号: HY-13749E
产品使用指南 技术支持

Sitagliptin (MK-0431) hydrochloride 是一种口服有效的且具有高选择性的 DPP4 抑制剂，其 IC50 值为 19 nM。Sitagliptin hydrochloride 通过竞争性抑制机制 (Kᵢ = 1 nM) 阻断 DPP-4 对胰高血糖素样肽-1 (GLP-1) 和葡萄糖依赖性胰岛素多肽 (GIP) 的降解，从而提升活性肠促胰岛素 (incretin) 水平。Sitagliptin hydrochloride 还可通过激活 cAMP/PKA 和 ERK1/2 通路，直接刺激肠道 L 细胞分泌 GLP-1，该作用独立于 DPP-4。Sitagliptin hydrochloride 在 1 型糖尿病模型中显示出对胰岛移植物的保护作用。Sitagliptin hydrochloride 可用于研究 1 型和 2 型糖尿病。

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Sitagliptin hydrochloride

Sitagliptin hydrochloride Chemical Structure

CAS No. : 486459-71-6

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Sitagliptin hydrochloride 的其他形式现货产品:

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Sitagliptin hydrochloride 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

生物活性

Sitagliptin (MK-0431) hydrochloride is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin hydrochloride blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin hydrochloride can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin hydrochloride shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin hydrochloride can be used for the study of 1-type and 2-type diabetes[1][2][3][4][5].

IC50 & Target[1][3]

DPP-4

19 nM (IC50)

ERK1

 

ERK2

 

分子量

443.77

Formula

C16H16ClF6N5O
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

Sitagliptin hydrochloride 相关分类

  • 摩尔计算器

  • 稀释计算器

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

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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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:

Sitagliptin486459-71-6MK-0431MK0431MK 0431Dipeptidyl PeptidaseGLP ReceptorEndogenous MetabolitePKAERKDPPProtein kinase AExtracellular signal regulated kinasesPharmacokineticsMetabolismDPP-IV InhibitionGLP-1 SecretionIslet Graft SurvivalInhibitorinhibitorinhibit

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