Sitagliptin

製品コードS5079 バッチS507903

印刷

化学情報

Chemical Structure Synonyms MK-0431 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C16H15F6N5O
分子量 407.31 CAS No. 486460-32-6
Solubility (25°C)* 体外 DMSO 81 mg/mL (198.86 mM)
Ethanol 81 mg/mL (198.86 mM)
Water 7 mg/mL (17.18 mM)
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Sitagliptin (MK-0431) is an oral and highly selective DPP-4 inhibitor with an IC50 of 18 nM. It is used for the treatment of type 2 diabetes.
in vitro Sitagliptin exhibits a > 2600-fold margin of selectivity against DPP8, DPP9, and other members of the dipeptidyl peptidase family (i.e., potency against DPP-4 vs. DPP8/9)[1]. This compound reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation[2]. It exerts a novel, direct action in order to stimulate GLP-1 secretion by the intestinal L cell through a DPP-4-independent, protein kinase A- and MEK-ERK1/2-dependent pathway. It therefore reduces the effect of autoimmunity on graft survival[3].
in vivo Sitagliptin is well absorbed after oral administration with a bioavailability of 87%. It has an apparent terminal half-life of 10–12 h at doses of 25-100 mg and is excreted mainly (≈ 80%) as unchanged compound by the kidneys. This compound does not interfere with the P450 cytochrome enzymes nor have there been any reported significant drug-drug interactions. It has been shown to inhibit DPP-4 activity by > 90% within 1-2 h of administration[1]. It has a short half-life in mice (1-2 h). Chronic sitagliptin treatment in a non-geneticmouse model of type 2 diabetes elicits significant improvement in glycemic control. The improved glucose homeostasis correlates with restoration of normal islet cell (α and β cells) mass, architecture and insulin secretion capacity in response to glucose stimulation[4]. This compound prolongs islet graft survival in streptozotocin-induced and NOD mice. Administration of this chemical in vivo reduces lymph node and splenic CD4+ T-cell migration, measured in vitro, via incretin- and nonincretin-mediated effects, respectively, and splenic sDPP-IV-responsive CD4+ T-cells and lymph node incretin nonresponsive CD4+ T-cells selectively infiltrated islets of diabetic NOD mice, after tail vein injection[5]. It significantly suppressed epileptogenesis in PTZ (pentylenetetrazole)-induced seizures. This compound counteracted neuronal damage and all biochemical, and histo-chemical alteration induced by PTZ. Oral sitagliptin can promote hippocampal neurogenesis, counteract hippocampal oxidative stress, and prevent the decline in mice cognition[6].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 CD4+ T-cells
濃度 100 μmol/l
反応時間 1 h
実験の流れ

CD4+ T-cells (1 × 106 cells) were plated on membrane inserts (8-μm pore size) in serum-free RPMI 1640 medium. Cell migration was assayed using Transwell chambers in media ± purified porcine kidney DPP-IV (32.1 units/mg; 100 mU/ml final concentration) ± this compound (100 μmol/l) or human GIP (100 nmol/l) or human GLP-1 (100 nmol/l). After 1 h, cells on the upper surface were removed mechanically and migrated cells in the lower compartment were counted.
動物実験 動物モデル male ICR mice
投薬量 280 mg/kg
投与方法 oral

参考

  • https://pubmed.ncbi.nlm.nih.gov/18182122/
  • https://pubmed.ncbi.nlm.nih.gov/19073764/
  • https://pubmed.ncbi.nlm.nih.gov/22186413/
  • https://pubmed.ncbi.nlm.nih.gov/19765579/
  • https://pubmed.ncbi.nlm.nih.gov/20368408/
  • https://pubmed.ncbi.nlm.nih.gov/29032011/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Elevated activity of plasma dipeptidyl peptidase 4 upon stress can be targeted to reverse tumor immunosuppression [ Pharmacol Res, 2025, 215:107696] PubMed: 40295089
DPP4-inhibition reduces pro-inflammatory cytokine production by alpha-beta and gamma-delta T cells in vitro and in the biliary atresia mouse model [ Sci Rep, 2025, 15(1):30226] PubMed: 40825831
Sitagliptin eye drops prevent the impairment of retinal neurovascular unit in the new Trpv2+/- rat model [ J Neuroinflammation, 2024, 21(1):312] PubMed: 39616390
Multiple Mechanisms of Action of Sulfodyne®, a Natural Antioxidant, against Pathogenic Effects of SARS-CoV-2 Infection [ Antioxidants (Basel), 2024, 13(9)1083] PubMed: 39334742
Untersuchungen zur Ursache der durch Dipeptidylpeptidase-4-Inhibitoren hervorgerufenen endothelialen Barrierestörung der Retina [ OPARU, 2024, 10.18725/OPARU-52005] PubMed: none
miR-23b-3p Ameliorates LPS-Induced Pulmonary Fibrosis by Inhibiting EndMT via DPP4 Inhibition [ Mol Biotechnol, 2023, 10.1007/s12033-023-00992-9] PubMed: 38150089
Multi-target mode of action of Sulfodyne®, a stabilized Sulforaphane, against pathogenic effects of SARS-CoV-2 infection [ bioRxiv, 2023, 10.1101/2023.12.18.572126] PubMed: none
Inhibition of CXXC5 function reverses obesity-related metabolic diseases [ Clin Transl Med, 2022, 12(4):e742] PubMed: 35384342
Nutritional control of thyroid morphogenesis through gastrointestinal hormones [ Curr Biol, 2022, S0960-9822(22)00137-3] PubMed: 35196509
A novel human stem cell-based biomarker assay for in vitro assessment of developmental toxicity [ Birth Defects Res, 2022, 10.1002/bdr2.2001] PubMed: 35289129

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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