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Purity: ≥98%
Teneligliptin HBr (formerly MP-513; MP513; trade name Tenelia in Japan), the hydrobromide salt of Teneligliptin, is a novel, potent, orally bioavailable and long-lasting dipeptidyl peptidase-4 (DPP-4) inhibitor; Teneligliptin is an approved drug for the treatment of type 2 diabetes mellitus in Japan. In vitro, it produced competitive inhibition against human plasma, rat plasma, and human recombinant DPP-4, with IC50 values of about 1 nM. While chronic teneligliptin treatment at doses ranging from 0.1 to 3.0 µmol/L does not decrease HUVEC cell viability, it does increase the expression of the heme oxygenase-1 (HMOX1) gene and decrease HG-stress markers in HUVEC cells cultured under hyperglycemia.
| Targets |
DPP4 (IC50 = 1 nM)
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| ln Vitro |
Teneligliptin (MP-513) exhibits concentration-dependent inhibition of all these DPP-4 enzymes. For rhDPP-4, human plasma, and rat plasma, the IC50s of teneligliptin are 0.889, 1.75, and 1.35 nM, respectively. Teneligliptin (MP-513) is investigated for its enzyme inhibition kinetics using rhDPP-4 as the enzyme source and Gly-Pro-MCA as the substrate. Teneligliptin (MP-513), according to plots based on the Michaelis-Menten equation, inhibits DPP-4 in a substrate-competitive manner; the residual sum of squares for the competitive and non-competitive models are, respectively, 0.162 and 0.192. The respective values of Ki, Km, and Vmax are 0.406 nM, 24 μM, and 6.06 nmol/min. GLP-1(7-36)amide is inhibited by teneligliptin (MP-513) with an IC50 of 2.92 nM[1].
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| ln Vivo |
Teneligliptin (MP-513) inhibits plasma DPP-4 in Wistar rats when given orally, with an ED50 of 0.41 mg/kg. Even 24 hours after taking teneligliptin, plasma DPP-4 inhibition remains intact (MP-513). In Zucker fatty rats, an oral carbohydrate-loading test demonstrates that Teneligliptin (MP-513) at ≥0.1 mg/kg decreases glucose excursions and increases the maximum increase in insulin and plasmaglucagon-like peptide-1 levels. After taking 1 mg/kg, this effect is seen over a period of 12 hours. Additionally, triglyceride and free fatty acid excursions are decreased by Teneligliptin (MP-513) at a dose of 1 mg/kg in an oral fat-loading test conducted on Zucker fatty rats. Teneligliptin (MP-513) is administered twice a week to Zucker fatty rats, which results in decreased plasma levels of free fatty acids and triglycerides during non-fasting periods and reduced glucose excursions in the oral carbohydrate-loading test. A dose-dependent inhibition of plasma DPP-4 is observed in rats upon oral administration of Teneligliptin (MP-513). As opposed to Sitagliptin and Vildagliptin, which have ED50 values of 27.3 and 12.8 mg/kg, respectively, Teneligliptin (MP-513) has an ED50 value of 0.41 mg/kg[1]. When hepatic lipogenesis-related genes are downregulated as a result of AMPK activation, teneligliptin (MP-513) improves the histopathological appearance of the liver and lowers intrahepatic triglyceride levels in an NAFLD model mouse[2].
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| Cell Assay |
HUVECs are seeded and given an overnight window to attach. The cells are subjected to three glucose experimental conditions the following day, with or without teneligliptin (at 0.1, 1.0, or 3.0 µmol/L) or sitagliptin (at 0.5 µmol/L): continuous normal glucose (NG-5 mmol/L) for 21 days; continuous high glucose (HG-25 mmol/L) for 21 days; or high-metabolic memory (HM-continuous HG for 14 days, followed by NG for the final 7 days). During the three weeks of culture, HUVECs are passedaging the cells and the medium is changed every 48 hours.
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| Animal Protocol |
Rats: Based on their body weight (306.2-374.2 g) and plasma DPP-4 activity, nine-week-old Wistar rats are randomly assigned to thirteen groups of eight animals each. Oral teneligliptin (MP-513) at doses of 0.01–0.1, 1–10 mg/mL/kg are given to four groups. All four groups are given sitagliptin and vildagliptin orally at doses of 0.1, 1, 10, and 100 mg/kg. One group receives an oral dose of the vehicle (0.5% hydroxypropyl methylcellulose). At 0 hours (pre-dose) and 0.5, 1, 2, 3, 6, 9, 12, and 24 hours (post-dose), blood samples are drawn from the tail vein using heparinized capillary tubes. The samples are then centrifuged at 1800 g for 15 minutes at 4°C. To measure DPP-4 activity, separated plasma is utilized. The dose of the inhibitors that produce half of the maximum effect, or ED50, is calculated for the dose-response curve using the maximum effect in each dose.
Mice: Newborn ICR mice are given a single subcutaneous injection of monosodium glutamate (MSG) at 4 mg/g body weight. Four weeks of age are used to split these mice into two groups of males: the MSG/HFD group (n = 6, Group 1) and the MSG/HFD/Teneligliptin (MP-513)-treated group (n = 6, Group 2). Group 2 mice receive Teneligliptin (MP-513) in their drinking water at 4 weeks of age (30 mg/kg per day). During the drug development process, data from animal experiments is used to determine the treatment dose of Teneligliptin (MP-513). Despite the fact that the dosage for the experimental animal is comparatively higher than what is used for humans in clinical practice, no appreciable side effects are seen during treatment. From 4 to 14 weeks of age, both groups receive a diet high in fruits and vegetables. To examine hepatic histopathology, all animals are killed by CO2 asphyxiation at the end of the experiment, which occurs at 14 weeks of age. |
| 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 |
C44H65BR5N12O2S2
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|---|---|
| Molecular Weight |
628.86
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| Exact Mass |
426.22
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| Elemental Analysis |
C, 42.02; H, 5.21; Br, 31.77; N, 13.36; O, 2.54; S, 5.10
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| CAS # |
906093-29-6
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| Related CAS # |
Teneligliptin;760937-92-6;Teneligliptin hydrobromide hydrate;1572583-29-9
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| PubChem CID |
11949652
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| Appearance |
Off-white to light brown solid powder
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| LogP |
8.461
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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 |
CC1=NN(C2C=CC=CC=2)C(N2CCN([C@@H]3CN[C@H](C(N4CSCC4)=O)C3)CC2)=C1.Br
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| InChi Key |
LUXIOMHUGCXFIU-MAYGPZJUSA-N
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| InChi Code |
InChI=1S/2C22H30N6OS.5BrH/c2*1-17-13-21(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*2-6,13,19-20,23H,7-12,14-16H2,1H3;5*1H/t2*19-,20-;;;;;/m00...../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;pentahydrobromide
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| Synonyms |
MP-513 hydrobromide; MP 513 hydrobromide; MP513 hydrobromide; Teneligliptin; trade name Tenelia; Teneligliptin HBr; Teneligliptin hydrobromide
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.98 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 (3.98 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 (3.98 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (159.02 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5902 mL | 7.9509 mL | 15.9018 mL | |
| 5 mM | 0.3180 mL | 1.5902 mL | 3.1804 mL | |
| 10 mM | 0.1590 mL | 0.7951 mL | 1.5902 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 |
| NCT05504239 | Recruiting | Drug: Teneligliptin 20 Mg Oral Tablet Drug: Teneligliptin Placebo Oral Tablet |
Type 2 Diabetes | Handok Inc. | October 2022 | Phase 3 |
| NCT05504226 | Recruiting | Drug: Teneligliptin 20 Mg Oral Tablet Drug: Teneligliptin Placebo Oral Tablet |
Type 2 Diabetes | Handok Inc. | October 2022 | Phase 3 |
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