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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.
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].
IC50 & Target
DPP-4
体外実験
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.
Suppressed c-Jun and c-Fos expression
Suppressed nuclear p65 protein accumulation
体内実験
Teneligliptin (0.1-1 mg/kg, p.o.) hydrobromide hydrate has excellent pharmacokinetic profile in rats and monkeys[1].
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
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.
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
6 months
-20°C
1 month
溶剤 & 溶解度
体外:
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)
Preparing Stock Solutions
ConcentrationSolventMass
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
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, 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.
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 (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 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 (5.86 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.
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.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
*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.
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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