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Teneligliptin (MP-513) hydrobromide 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 improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus.
For research use only. We do not sell to patients.
Teneligliptin (MP-513) hydrobromide 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 improves blood glucose levels and can be used in researches related to type 2 diabetes mellitus[1][2][3][4][5][6][7][8].
Teneligliptin (2.5-5 μM, 24 h) hydrobromide 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 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 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 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 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 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.
Suppressed c-Jun and c-Fos expression
Suppressed nuclear p65 protein accumulation
In Vivo
Teneligliptin (0.1-1 mg/kg, p.o.) hydrobromide has excellent pharmacokinetic profile in rats and monkeys[1].
Teneligliptin (10 mg/kg, p.o., 24 weeks) hydrobromide 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 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 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 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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Diabetic cardiomyopathy (55 mg/kg STZ (HY-13753) was administered to C57BL/6 male mice by intraperitoneal injection for 5 consecutive days, fasting blood glucose level was higher than 16.7 mmol/L)[3]
Dosage:
30 mg/kg
Administration:
Oral gavage (p.o.), 4 weeks
Result:
Ameliorated myocardial hypertrophy.
Improved heart function, with increasing the fractional shortening to 49.6%.
Reduced the expression of myocardial injury indicators (CK-MB, AST, LDH).
Reduced the critical pathological factor NOX4.
Reduced activation of the NLRP3 inflammasome and IL-1β in the heart.
DMSO : ≥ 100 mg/mL (159.02 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
*"≥" means soluble, but saturation unknown.
Preparing Stock Solutions
ConcentrationSolventMass
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
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
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.
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO 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 (3.98 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 μLDMSO 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.
Protocol 3
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn oil, and mix evenly.
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. 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: PBS
Solubility: 100 mg/mL (159.02 mM); Clear solution; Need ultrasonic
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.
Calculation results:
Working solution concentration:
mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
*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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO / H2O
1 mM
1.5902 mL
7.9509 mL
15.9018 mL
39.7545 mL
5 mM
0.3180 mL
1.5902 mL
3.1804 mL
7.9509 mL
10 mM
0.1590 mL
0.7951 mL
1.5902 mL
3.9754 mL
15 mM
0.1060 mL
0.5301 mL
1.0601 mL
2.6503 mL
20 mM
0.0795 mL
0.3975 mL
0.7951 mL
1.9877 mL
25 mM
0.0636 mL
0.3180 mL
0.6361 mL
1.5902 mL
30 mM
0.0530 mL
0.2650 mL
0.5301 mL
1.3251 mL
40 mM
0.0398 mL
0.1988 mL
0.3975 mL
0.9939 mL
50 mM
0.0318 mL
0.1590 mL
0.3180 mL
0.7951 mL
60 mM
0.0265 mL
0.1325 mL
0.2650 mL
0.6626 mL
80 mM
0.0199 mL
0.0994 mL
0.1988 mL
0.4969 mL
100 mM
0.0159 mL
0.0795 mL
0.1590 mL
0.3975 mL
*
Note: If you choose water as the stock solution, please dilute it to the working solution,
then filter and sterilize it with a 0.22 μm filter before use.
Teneligliptin hydrobromide Related Classifications
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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