Teneligliptin
Based on 6 publication(s) in Google Scholar
Teneligliptin (MP-513) hydrobromide hydrate is an orally active and selective dipeptidyl peptidase 4 (DPP-4) inhibitor (IC50s: 0.37 and 0.29 nM for the human and rat DPP-4, respectively). Teneligliptin hydrobromide hydrate improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus.
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: 99.79%
- CAS 番号: 760937-92-6
- 分子式: C22H30N6OS
- 分子量:426.58
-
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]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Metabolism/Protease Compound Library
HY-L012
-
FDA-Approved Drug Library
HY-L022
-
Anti-Aging Compound Library
HY-L034
-
Drug Repurposing Compound Library
HY-L035
-
Anti-diabetic Compound Library
HY-L040
-
Oxygen Sensing Compound Library
HY-L045
-
Endocrinology Compound Library
HY-L047
-
Ferroptosis Compound Library
HY-L051
-
Pyroptosis Compound Library
HY-L059
-
Orally Active Compound Library
HY-L061
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Human Metabolite Library
HY-L123
-
Heterocyclic Compound Library
HY-L138
-
Metabolic Enzyme Compound Library
HY-L146
-
Protease Inhibitor Library
HY-L147
-
Highly Selective Inhibitors Library
HY-L158
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
Bioactive Compound Library
HY-L001
-
Amino Acid Metabolism Compound Library
HY-L189
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
MedChemExpress（MCE）の使用を引用している文献 Teneligliptin
More- Nephrol Dial Transplant. 2019 Oct 1;34(10):1669-1680. [Abstract]
- Antioxidants (Basel). 2023 Jul 24;12(7):1478. [Abstract]
- Antioxidants (Basel). 2021 Sep 9;10(9):1438. [Abstract]
- Eur J Med Chem. 2021 Feb 15;212:113030. [Abstract]
- Cosmetics. 2024 Mar 1, 11(2), 35.
- Chem Res Toxicol. 2020 Aug 17;33(8):2164-2171. [Abstract]
生物活性
|
DPP-4 |
Teneligliptin (2.5-5 μM, 24 h) hydrobromide hydrate prevents activation of the NLRP3 inflammasome and injury by increasing the phosphorylation of AMPK in primary mouse cardiomyocytes treated with high glucose[3].
Teneligliptin (1-3 μM, 12 h) hydrobromide hydrate protects against hypoxia/reoxygenation-induced endothelial cell injury in rat cardiac microvascular endothelial cells, with suppressing reactive oxygen species (ROS) production[5].
Teneligliptin (1.5-3 μM, 24 h) hydrobromide hydrate prevents Doxorubicin (HY-15142A)-induced inflammation (cytokines, including MCP-1 and IL-1β) and Apoptosis (improvement of the Bax/Bcl-2 ratio) in H9c2 cells[6].
Teneligliptin (2.5-5 μM, 2-48 h) hydrobromide hydrate inhibits Lipopolysaccharide-induced cytotoxicity and inflammation through inhibiting TLR4 and JNK/AP1/NF-κB signaling in dental pulp cells, with reducing oxidative stress[7].
Teneligliptin (3 μM, 3 h) hydrobromide hydrate prevents high glucose and H2O2 induced USP22-SIRT1 downregulation by p38MAPK inhibition and inhibits high glucose induced mitochondrial dysfunction, beta cell apoptosis as well as insulin secretion decreases in INS-1 cells[8].
Teneligliptin (3 μM, 3 h) hydrobromide hydrate inhibits high glucose induced mitochondrial dysfunction by SIRT1 activation in human 1.1b4 beta cells[8].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Primary mouse cardiomyocytes treated with high glucose (30 mmol/L)
-
Concentration:2.5, 5 μM
-
Incubation Time:24 h
-
Result:Inhibited NLRP3 and caspase-1 at 2.5 and 5 µM.
Increased the p-AMPK.
-
Cell Line:Cardiac microvascular endothelial cells isolated from 1- to 4-day-old SD rats
-
Concentration:1, 3 μM
-
Incubation Time:12 h
-
Result:Suppressed reactive oxygen species (ROS) and the vascular adhesion molecule ICAM-1.
Suppressed transcriptional factor Egr-1 expression.
-
Cell Line:Human dental pulp cells
-
Concentration:2.5, 5 μM
-
Incubation Time:24 h
-
Result:Suppressed c-Jun and c-Fos expression
Suppressed nuclear p65 protein accumulation
Teneligliptin (10 mg/kg, p.o., 24 weeks) hydrobromide hydrate ameliorates diabetic polyneuropathy and inhibits glucose-stimulated blood glucose elevation by increasing pancreatic β-cell volume density (Vβ), insulin secretion in spontaneously type 2 diabetic rats[2].
Teneligliptin (30 mg/kg, p.o., 4 weeks) hydrobromide hydrate attenuates myocardial hypertrophy, injury and associated inflammatory response in STZ (HY-13753)-induced diabetic cardiomyopathy mice by inhibiting NLRP3 inflammasome activation[3].
Teneligliptin (30-60 mg/kg, drinking water, 10 weeks) hydrobromide hydrate prevents obesity and obesity-related manifestations with increased energy expenditure in a mouse model of high-fat diet-induced obesity (inhibition of adipocyte hypertrophy, hepatic steatosis)[4].
Pharmacokinetics properties of teneligliptin hydrobromide hydrate by oral administration
| Animal | Dose (mg/kg) | tmax (h) | Cmax (ng/mL) | t1/2 (h) | AUC0-last (h × ng/mL) | BA (%) | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Rat | 0.1 | 0.88 | 5.48 | 15.84 | 91.81 | 85.9 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Rat | 0.3 | 0.75 | 20.65 | 8.97 | 202.12 | 63 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Rat | 1 | 0.75 | 152.41 | 8.43 | 672.94 | 62.9 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Monkey | 0.1 | 0.5 | 28.27 | 18.86 | 295.44 | 83.2 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Monkey | 0.3 | 1.38 | 85.13 | 15.24 | 613.16 | 57.6 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Monkey | 1 | 0.88 | 273.54 | 16.11 | 1571.64 | 44.1 |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 760937-92-6
-
性状 Solid
-
分子量 426.58
-
分子式 C22H30N6OS
-
Color White to off-white
-
SMILES
O=C([C@H]1NC[C@@H](N2CCN(C3=CC(C)=NN3C4=CC=CC=C4)CC2)C1)N5CSCC5
-
別名
MP-513
-
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 2 years -20°C 1 year
Publications (6)
-
Journal Impact Factor
-
Most Recent
-
Nephrol Dial Transplant
Dipeptidyl peptidase-4 inhibitor teneligliptin accelerates recovery from cisplatin-induced acute kidney injury by attenuating inflammation and promoting tubular regeneration. [Abstract]2019 Oct 1;34(10):1669-1680. PMID: 30624740 -
Antioxidants (Basel)
Teneligliptin Co-Infusion Alleviates Morphine Tolerance by Inhibition of Spinal Microglial Cell Activation in Streptozotocin-Induced Diabetic Rats. [Abstract]2023 Jul 24;12(7):1478. PMID: 37508016 -
Antioxidants (Basel)
Teneligliptin Exerts Antinociceptive Effects in Rat Model of Partial Sciatic Nerve Transection Induced Neuropathic Pain. [Abstract]2021 Sep 9;10(9):1438. PMID: 34573072 -
Eur J Med Chem
2021 Feb 15;212:113030. PMID: 33248849 -
-
Chem Res Toxicol
Teneligliptin Promotes Bile Acid Synthesis and Attenuates Lipid Accumulation in Obese Mice by Targeting the KLF15-Fgf15 Pathway. [Abstract]2020 Aug 17;33(8):2164-2171. PMID: 32639145
溶剤 & 溶解度
DMSO : 100 mg/mL (234.42 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)
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 (5.86 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 (5.86 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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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
-
データシート (300 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Yoshida T, et al. Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Bioorg Med Chem. 2012 Oct 1;20(19):5705-19. [Content Brief]
[2]. Guo D, et al. Beneficial effects of combination therapy of canagliflozin and teneligliptin on diabetic polyneuropathy and β-cell volume density in spontaneously type 2 diabetic Goto-Kakizaki rats. Metabolism. 2020 Jun;107:154232. [Content Brief]
[3]. Zhang GL, et al. Teneligliptin mitigates diabetic cardiomyopathy by inhibiting activation of the NLRP3 inflammasome. World J Diabetes. 2024 Apr 15;15(4):724-734. [Content Brief]
[4]. Fukuda-Tsuru S, et al. The novel dipeptidyl peptidase-4 inhibitor teneligliptin prevents high-fat diet-induced obesity accompanied with increased energy expenditure in mice. Eur J Pharmacol. 2014 Jan 15;723:207-15. [Content Brief]
[5]. Zhang Z, et al. Teneligliptin protects against hypoxia/reoxygenation-induced endothelial cell injury. Biomed Pharmacother. 2019 Jan;109:468-474. [Content Brief]
[6]. Peng W, et al. Teneligliptin prevents doxorubicin-induced inflammation and apoptosis in H9c2 cells. Arch Biochem Biophys. 2020 Apr 15;683:108238. [Content Brief]
[7]. Liu X, et al. Teneligliptin inhibits lipopolysaccharide-induced cytotoxicity and inflammation in dental pulp cells. Int Immunopharmacol. 2019 Aug;73:57-63. [Content Brief]
[8]. Elumalai S, et al. High glucose-induced PRDX3 acetylation contributes to glucotoxicity in pancreatic β-cells: Prevention by Teneligliptin. Free Radic Biol Med. 2020 Nov 20;160:618-629. [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 | 2.3442 mL | 11.7211 mL | 23.4423 mL | 58.6057 mL |
| 5 mM | 0.4688 mL | 2.3442 mL | 4.6885 mL | 11.7211 mL | |
| 10 mM | 0.2344 mL | 1.1721 mL | 2.3442 mL | 5.8606 mL | |
| 15 mM | 0.1563 mL | 0.7814 mL | 1.5628 mL | 3.9070 mL | |
| 20 mM | 0.1172 mL | 0.5861 mL | 1.1721 mL | 2.9303 mL | |
| 25 mM | 0.0938 mL | 0.4688 mL | 0.9377 mL | 2.3442 mL | |
| 30 mM | 0.0781 mL | 0.3907 mL | 0.7814 mL | 1.9535 mL | |
| 40 mM | 0.0586 mL | 0.2930 mL | 0.5861 mL | 1.4651 mL | |
| 50 mM | 0.0469 mL | 0.2344 mL | 0.4688 mL | 1.1721 mL | |
| 60 mM | 0.0391 mL | 0.1954 mL | 0.3907 mL | 0.9768 mL | |
| 80 mM | 0.0293 mL | 0.1465 mL | 0.2930 mL | 0.7326 mL | |
| 100 mM | 0.0234 mL | 0.1172 mL | 0.2344 mL | 0.5861 mL |
Teneligliptin 関連分類
HY-14806 関連分類
Powered by Bioz