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| 25mg |
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Teneligliptin (MP513; trade name Tenelia in Japan) is a novel, potent, orally bioavailable and long-lasting dipeptidyl peptidase-4 (DPP-4) inhibitor; it competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM. Chronic teneligliptin treatment at doses between 0.1 and 3.0 µmol/L does not reduce cell viability of HUVECs, but decreases HG-stress markers and increases heme oxygenase-1 (HMOX1) gene expression in HUVEC cells incubated under hyperglycemia. Teneligliptin is an approved drug for the treatment of type 2 diabetes mellitus in Japan.
| ln Vitro |
All of these DPP-4 enzymes are inhibited by teneligliptin (MP-513) in a concentration-dependent manner. Teneligliptin (MP-513) has an IC50 of 0.889, 1.75, and 1.35 nM against rhDPP-4, human plasma, and rat plasma, respectively. Teneligliptin (MP-513) was used as the enzyme source and Gly-Pro-MCA as the substrate in an investigation of the kinetics of enzyme inhibition. Teneligliptin (MP-513) inhibits DPP-4 in a substrate-competitive manner, according to plots based on the Michaelis-Menten equation; the residual sums of squares for the competitive and noncompetitive models were 0.162 and 0.192, respectively. The values of Ki, Km, and Vmax are 6.06 nmol/min, 24 μM, and 0.406 nM, respectively. With an IC50 of 2.92 nM, teneligliptin (MP-513) inhibits the breakdown of GLP-1(7-36)amide[1].
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| ln Vivo |
Teneligliptin (MP-513) has an ED50 of 0.41 mg/kg and can inhibit plasma DPP-4 when given orally to Wistar rats. Even 24 hours after the dose of teneligliptin (MP-513) there was still suppression of plasma DPP-4. Teneligliptin (MP-513) at ≥0.1 mg/kg maximally enhanced plasma glucagon-like peptide-1 and insulin levels and decreased blood glucose excursions in Zucker adipose rats, according to an oral carbohydrate loading test. Within 12 hours of ingesting a dose of 1 mg/kg, this effect is seen. Additionally, triglyceride and free fatty acid excursions were decreased by teneligliptin (MP-513) at a dose of 1 mg/kg in an oral fat loading test conducted on Zucker adipose rats. Teneligliptin (MP-513) was administered twice a week for two weeks in Zucker fatty rats. This treatment decreased plasma triglyceride and free fatty acid levels while the animals were not fasting. It also decreased glucose excursions in an oral carbohydrate loading test. Rat plasma DPP-4 is inhibited by oral treatment of Teneligliptin (MP-513) in a dose-dependent manner. Teneligliptin (MP-513) was shown to have an ED50 value of 0.41 mg/kg, whereas sitagliptin and vildagliptin had ED50 values of 27.3 and 12.8 mg/kg, respectively[1]. Teneligliptin (MP-513) is associated with the downregulation of hepatic lipogenesis-related genes brought on by AMPK activation, which enhances the histological appearance of the liver and lowers intrahepatic triglyceride levels in NAFLD model mice [2].
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| References |
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| Additional Infomation |
Teneligliptin is an amino acid amide.
Teneligliptin has been investigated for the treatment of Type 2 Diabetes Mellitus. Teneligliptin is a long-acting, orally bioavailable, pyrrolidine-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. Teneligliptin may also reduce plasma triglyceride levels through a sustained increase in GLP-1 levels. |
| Molecular Formula |
C22H30N6OS
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|---|---|
| Molecular Weight |
426.58
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| Exact Mass |
426.22
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| CAS # |
760937-92-6
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| Related CAS # |
Teneligliptin hydrobromide;906093-29-6;Teneligliptin hydrobromide hydrate;1572583-29-9;Teneligliptin-d8;1391012-95-5;Teneligliptin-d4
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| PubChem CID |
11949652
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
663.4±55.0 °C at 760 mmHg
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| Flash Point |
355.0±31.5 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.721
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| LogP |
1.15
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
594
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O=C([C@H]1NC[C@@H](N2CCN(C3=CC(C)=NN3C4=CC=CC=C4)CC2)C1)N5CSCC5
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| InChi Key |
WGRQANOPCQRCME-PMACEKPBSA-N
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| InChi Code |
InChI=1S/C22H30N6OS/c1-17-13-21(28(24-17)18-5-3-2-4-6-18)26-9-7-25(8-10-26)19-14-20(23-15-19)22(29)27-11-12-30-16-27/h2-6,13,19-20,23H,7-12,14-16H2,1H3/t19-,20-/m0/s1
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| Chemical Name |
[(2S,4S)-4-[4-(5-methyl-2-phenylpyrazol-3-yl)piperazin-1-yl]pyrrolidin-2-yl]-(1,3-thiazolidin-3-yl)methanone
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~78.13 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.86 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3442 mL | 11.7211 mL | 23.4423 mL | |
| 5 mM | 0.4688 mL | 2.3442 mL | 4.6885 mL | |
| 10 mM | 0.2344 mL | 1.1721 mL | 2.3442 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04431141 | COMPLETED | Drug: Teneligliptin Drug: Empagliflozin Drug: Teneligliptin and Empagliflozin |
Type 2 Diabetes Mellitus | Handok Inc. | 2020-09-15 | Phase 1 |
| NCT03769870 | COMPLETED | Drug: Teneligliptin 20mg/day Drug: Atorvastatin 40mg/Day Drug: Teneligliptin 20mg/day + Atorvastatin 40mg/day |
Diabete Mellitus | Handok Inc. | 2019-01-11 | Phase 1 |
| NCT03009513 | COMPLETED | Drug: Teneligliptin+Glimepiride | Diabetes Mellitus | Handok Inc. | 2017-01 | Phase 1 |
| NCT02449330 | UNKNOWN STATUS | Drug: Teneligliptin | Diabetes Mellitus, Type 2 | National Cerebral and Cardiovascular Center, Japan | 2015-06 | Phase 4 |
| NCT02314637 | COMPLETEDWITH RESULTS | Drug: Teneligliptin Drug: Teneligliptin + Sulfonylurea |
Type 2 Diabetes Mellitus | Mitsubishi Tanabe Pharma Corporation | 2009-08 | Phase 3 |
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