アナグリプチン
Based on 3 publication(s) in Google Scholar
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。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.92%
- CAS 番号: 739366-20-2
- 分子式: C19H25N7O2
- 分子量:383.45
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Anagliptin
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生物活性
製品説明
IC50 & Target
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DPP-4 3.8 nM (IC50) |
DPP-9 60 nM (IC50) |
DPP-8 68 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | IC50 |
176700 nM
Compound: Anagliptin
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Inhibition of DPP-2 expressed in human Caco-2 cells using H-Lys-Ala-AMC as substrate preincubated for 30 mins before substrate addition measured after 20 mins by fluorescence assay
Inhibition of DPP-2 expressed in human Caco-2 cells using H-Lys-Ala-AMC as substrate preincubated for 30 mins before substrate addition measured after 20 mins by fluorescence assay
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[PMID: 22019046] |
| Sf9 | IC50 |
72700 nM
Compound: Anagliptin
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Inhibition of human recombinant FAP expressed in baculovirus-infected Sf9 insect cells using H-Ala-Pro-AFC as substrate after 60 mins by fluorescence assay
Inhibition of human recombinant FAP expressed in baculovirus-infected Sf9 insect cells using H-Ala-Pro-AFC as substrate after 60 mins by fluorescence assay
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[PMID: 22019046] |
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.
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Cell Line:Rat smooth muscle cells (SMC)
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Concentration:1, 10 and 100 μM
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Incubation Time:24 h
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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.
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Cell Line:Rat smooth muscle cells (SMC)
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Concentration:100 μM
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Incubation Time:10 min
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Result:Blocked the early- but not the late-phase ERK phosphorylation induced by s-DPP-4.
体内実験
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.
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Animal Model:Male apoliporotein E (apoE)-deficient mice[2]
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Dosage:0.3%
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Administration:In diet, 16 weeks
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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.
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Animal Model:Male low‐density lipoprotein receptor‐deficient mice (B6.129S7‐Ldlrtm1Her/J)[3]
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Dosage:0.3%
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Administration:In diet, 4 weeks
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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.
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Animal Model:Male Sprague–Dawley rats and Beagle dogs[1]
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Dosage:0.2, 0.5, 1 and 10 mg/kg
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Administration:Oral or intravenous administration (Pharmacokinetic Studies)
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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
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 739366-20-2
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性状 Solid
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分子量 383.45
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分子式 C19H25N7O2
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Color White to yellow
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SMILES
O=C(C1=CN2C(N=C1)=CC(C)=N2)NCC(C)(NCC(N3[C@H](C#N)CCC3)=O)C
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別名
Anagliptin; SK-0403
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Biochem Pharmacol
Identification of a novel metabolite of vildagliptin in humans: Cysteine targets the nitrile moiety to form a thiazoline ring. [Abstract]2018 Oct:156:312-321. PMID: 30172711 -
Mol Med Rep
The effect of anagliptin on intimal hyperplasia of rat carotid artery after balloon injury. [Abstract]2017 Dec;16(6):8003-8010. PMID: 28990108 -
Exp Ther Med
Anagliptin promotes apoptosis in mouse colon carcinoma cells via MCT-4/lactate-mediated intracellular acidosis. [Abstract]2022 Apr;23(4):282. PMID: 35317435
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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データシート (281 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Kato N, et al. Discovery and pharmacological characterization of N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor. Bioorg Med Chem. 2011 Dec 1;19(23):7221-7. [Content Brief]
[2]. Ervinna N, et al. Anagliptin, a DPP-4 inhibitor, suppresses proliferation of vascular smooth muscles and monocyte inflammatory reaction and attenuates atherosclerosis in male apo E-deficient mice. Endocrinology. 2013 Mar;154(3):1260-70. [Content Brief]
[3]. Yano W, et al. Mechanism of lipid-lowering action of the dipeptidyl peptidase-4 inhibitor, anagliptin, in low-density lipoprotein receptor-deficient mice. J Diabetes Investig. 2017 Mar;8(2):155-160. [Content Brief]
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 |
Anagliptin 関連分類
HY-14877 関連分類
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