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

Anagliptin  (Synonyms: SK-0403)

製品番号: HY-14877 純度: 99.91%
COA 取扱説明書

Anagliptin (SK-0403) is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC50s of 68 nM and 60 nM, respectively.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 127 在庫あり
Solution
10 mM * 1 mL in DMSO USD 127 在庫あり
Solid
5 mg USD 115 在庫あり
10 mg USD 190 在庫あり
50 mg USD 610 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

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カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Other Forms of Anagliptin:

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Dipeptidyl Peptidase アイソフォーム固有の製品をすべて表示:

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製品説明

Anagliptin (SK-0403) is a highly selective, potent, orally active inhibitor of dipeptidyl peptidase 4 (DPP-4), with an IC50 of 3.8 nM, and less selective at DPP-8 and DDP-9 with IC50s of 68 nM and 60 nM, respectively[1].

IC50 & Target

DPP-4

3.8 nM (IC50)

DPP-9

60 nM (IC50)

DPP-8

68 nM (IC50)

体外実験

Anagliptin (SK-0403) (0-100 μM; 24 h) attenuates s-DPP-4-induced smooth muscle cells proliferation[2].
Anagliptin (100 μM; 10 min) reduces TNF-α production in cultured monocytes[2].
Anagliptin (0.001-10 μM; 24 h) significantly suppresses sterol regulatory element‐binding protein activity in HepG2 cells (21% decrease)[3].

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

Cell Proliferation Assay[2]

Cell Line: Rat smooth muscle cells (SMC)
Concentration: 1, 10 and 100 μM
Incubation Time: 24 h
Result: Attenuated s-DPP-4-induced SMC proliferation in a dose-dependent manner. Inhibited LPS-induced ERK phosphorylation and markedly suppressed LPS-induced nuclear translocation of NF-κBp65.

Western Blot Analysis[2]

Cell Line: Rat smooth muscle cells (SMC)
Concentration: 100 μM
Incubation Time: 10 min
Result: Blocked the early- but not the late-phase ERK phosphorylation induced by s-DPP-4.
体内実験

Anagliptin (SK-0403) (0.3%; in diet; 16 weeks) reduces atherosclerotic lesion and does not increase the number of circulating EPCs in apoliporotein E (apoE)-deficient mice[2].
Anagliptin (0.3%; in diet; 4 weeks) exhibits a lipid‐lowering effect in a hyperlipidemic mice model[3].

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

Animal Model: Male apoliporotein E (apoE)-deficient mice[2]
Dosage: 0.3%
Administration: In diet, 16 weeks
Result: Reduced DPP-4 activity in the plasma as expected and did not affect food consumption or body weight gain. Significantly reduced total cholesterol level, especially VLDL and LDL-C without affecting triglyceride level. Also decreased the α-SMA-positive area within the individual plaque.
Animal Model: Male low‐density lipoprotein receptor‐deficient mice (B6.129S7‐Ldlrtm1Her/J)[3]
Dosage: 0.3%
Administration: In diet, 4 weeks
Result: Significantly decreased the plasma total cholesterol (14% reduction) and triglyceride levels (27% reduction). Significantly decreased low‐density lipoprotein cholesterol and very low‐density lipoprotein cholesterol. Sterol regulatory element‐binding protein‐2 messenger ribonucleic acid expression level was significantly decreased at night.
Animal Model: Male Sprague–Dawley rats and Beagle dogs[1]
Dosage: 0.2, 0.5, 1 and 10 mg/kg
Administration: Oral or intravenous administration (Pharmacokinetic Studies)
Result: Selected PK parameters of Anagliptin hydrochloride in rats and dogs[1]
Compound Species CLtot
(l/h/kg)
Vdss
(l/h/kg)
Cmaxc
(ng/ml)
Tmaxc
(h)
T1/2
(h)
AUC
(ng/h/ml)
BA
(%)
Anagliptin hydrochloridea Rat 2.00 (iv) 0.68 (iv) 309 (62) (po) 0.8 (2.3) (po) 1.9 (po) 1160 (po) 23 (po)
Dog 0.65 (iv) 0.83 (iv) 261 (po) 1.5 (po) 1.0 (po) 824 (po) 100 (po)

aAnagliptin hydrochloride dose in rats, 1 mg/kg, iv (n = 3); 10 mg/kg, po (n = 3). 4a dose in dogs, 0.2 mg/kg, iv (n = 3); 0.5 mg/kg, po (n = 2). cValues in parentheses were obtained at a dose of 3 mg/kg (n = 3).
臨床実験
分子量

383.45

分子式

C19H25N7O2

CAS 番号
Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=CN2C(N=C1)=CC(C)=N2)NCC(C)(NCC(N3[C@H](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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6079 mL 13.0395 mL 26.0790 mL 65.1975 mL
5 mM 0.5216 mL 2.6079 mL 5.2158 mL 13.0395 mL
10 mM 0.2608 mL 1.3040 mL 2.6079 mL 6.5198 mL
15 mM 0.1739 mL 0.8693 mL 1.7386 mL 4.3465 mL
20 mM 0.1304 mL 0.6520 mL 1.3040 mL 3.2599 mL
25 mM 0.1043 mL 0.5216 mL 1.0432 mL 2.6079 mL
30 mM 0.0869 mL 0.4347 mL 0.8693 mL 2.1733 mL
40 mM 0.0652 mL 0.3260 mL 0.6520 mL 1.6299 mL
50 mM 0.0522 mL 0.2608 mL 0.5216 mL 1.3040 mL
60 mM 0.0435 mL 0.2173 mL 0.4347 mL 1.0866 mL
80 mM 0.0326 mL 0.1630 mL 0.3260 mL 0.8150 mL
100 mM 0.0261 mL 0.1304 mL 0.2608 mL 0.6520 mL
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Anagliptin Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (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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製品名:
Anagliptin
製品番号:
HY-14877
数量:
MCE 日本正規代理店: