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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.
For research use only. We do not sell to patients.
Teneligliptin hydrobromide hydrate Chemical Structure
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[1][2][3][4][5][6][7][8].
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.
Teneligliptin hydrobromide hydrate Related Antibodies
Suppressed c-Jun and c-Fos expression
Suppressed nuclear p65 protein accumulation
In Vivo
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].
Teneligliptin (0.1-1 mg/kg, p.o.) hydrobromide hydrate has excellent pharmacokinetic profile in rats and monkeys[1]. 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
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.
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.
This equation is commonly abbreviated as: C1V1 = C2V2
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
H2O
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
*
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 hydrate 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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