1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase
  3. Anagliptin

Anagliptin (Synonyms: SK-0403)

製品番号: HY-14877 純度: 97.96%
取扱説明書

Anagliptin is a highly selective, potent inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8/9 (IC50, 68, 60 nM, respectively).

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Anagliptin 構造式

Anagliptin 構造式

CAS 番号 : 739366-20-2

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 154 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 140 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 240 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 950 在庫あり
Estimated Time of Arrival: December 31
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 2 publication(s) in Google Scholar

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製品説明

Anagliptin is a highly selective, potent inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8/9 (IC50, 68, 60 nM, respectively).

IC50 & Target

IC50: 3.8 nM (DPP-4), 68 nM (DPP-8), 60 nM (DPP-9)[1]

体外実験

Anagliptin is a highly selective, potent inhibitor of DPP-IV, with an IC50 of 3.8 nM, and less selective at DPP-8/9 (68, 60 nM, respectively). Anagliptin does not affect CYP3A4, CYP2C19, CYP2C9, CYP1A2, and CYP2D6 (IC50 >10 μM) or CYP3A4, CYP2C8, CYP2C9, and CYP1A2 at 50 μM. Anagliptin hydrochloride does not bind to the hERG channel (E-4031, >90% inhibition at 0.1 μM, IC50 >500 μM in patch clamp using HEK 293 cells)[1]. Anagliptin (1-100 μM) dose-dependently suppresses-DPP-4-induced smooth muscle cells (SMCs) proliferation, and reduces TNF-α production in cultured monocytes[2].

体内実験

Anagliptin (0.3%) alters the quantity and quality of atherosclerotic lesions in apoE-deficient mice, and reduces DPP-4 activity in the plasma, and total cholesterol level, especially VLDL and LDL-C in mice. Anagliptin also decreases α-SMA-positive area and TNF-α-positive lesions in plaque area of apoE-deficient mice. In addition, Anagliptin does not increase the number of circulating endothelial progenitor cells (EPCs) in apoE-deficient mice[2]. Anagliptin (0.3%) decreases the low-density lipoprotein cholesterol and very low-density lipoprotein cholesterol, and also reduces the sterol regulatory element-binding protein-2 messenger ribonucleic acid expression level in mice[3].

臨床実験
分子量

383.45

分子式

C₁₉H₂₅N₇O₂

CAS 番号

739366-20-2

SMILES

O=C(C1=CN2C(N=C1)=CC(C)=N2)NCC(C)(NCC(N3[[email protected]](C#N)CCC3)=O)C

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (260.79 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6079 mL 13.0395 mL 26.0790 mL
5 mM 0.5216 mL 2.6079 mL 5.2158 mL
10 mM 0.2608 mL 1.3040 mL 2.6079 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
細胞実験
[2]

To evaluate the growth response of cultured smooth muscle cells (SMCs) to s-DPP-4, the bromodeoxyuridine (BrdU) incorporation assay is performed using cell proliferation ELISA kit. Briefly, SMCs are plated at a density of 3000 cells/well in 96-well culture plates with complete media. At 60%-70% confluence, the SMCs are pretreated with or without 1, 10 or 100 μM Anagliptin for 10 minutes and finally stimulated with soluble recombinant human (rh) DPP-4 (5 to 500 ng/mL) for 20 hours. Then, BrdU solution (10 μM) is added to the cells and the cells are cultured for another 4 hours. Then, the cells are dried and fixed, and the cellular DNA is denatured with FixDenat solution for 30 minutes at room temperature. A rat anti-BrdU monoclonal antibody conjugated with peroxidase is added to the culture plates and incubated again at room temperature for 90 minutes. Finally, tetramethylbenzidine is added before incubation for 15 minutes at room temperature. Absorbance is measured by a microplate reader at 370 nm[2].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[2]

Mice[2]
Male apoliporotein E (apoE)-deficient mice and C57BL/6 mice at the age of 7 weeks, are housed in specific pathogen-free barrier facilities. Mice are maintained under 12-hour light/dark cycle, and fed a standard rodent diet (22.6% protein, 53.8% carbohydrate, 5.6% fat, 6.6% mineral and vitamin mixture, and 3.3% fiber; total, 356 kcal/100 g) with water ad libitum. At the age of 9 weeks, apoE-deficient mice are fed Anagliptin-containing diet (0.3%, Anagliptin group, n = 30) or DPP-4 inhibitor-free diet (control group n = 30) for 16 weeks[2].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献
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Keywords:

AnagliptinSK-0403SK0403SK 0403Dipeptidyl PeptidaseDPPInhibitorinhibitorinhibit

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製品名:
Anagliptin
製品番号:
HY-14877
数量:
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