Teneligliptin hydrobromide hydrate
Based on 6 publication(s) in Google Scholar
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.
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- Pureza : 99.97%
- No. CAS: 1572583-29-9
- Fòrmula: C22H30N6OS·xH2O·2.5Br
- Peso molecular:426.58 (free base)
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Publications Citing Use of MedChemExpress (MCE) Teneligliptin hydrobromide hydrate
More- Nephrol Dial Transplant. 2019 Oct 1;34(10):1669-1680. [Abstract]
- Antioxidants (Basel). 2023 Jul 24;12(7):1478. [Abstract]
- Antioxidants (Basel). 2021 Sep 9;10(9):1438. [Abstract]
- Eur J Med Chem. 2021 Feb 15:212:113030. [Abstract]
- Cosmetics. 2024 Mar 1, 11(2), 35.
- Chem Res Toxicol. 2020 Aug 17;33(8):2164-2171. [Abstract]
Ver todos los productos específicos de isoformas AMPK
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Actividad biológica
Descripciòn
|
TLR4 |
NLRP3 inflammasome |
DPP-4 |
In Vitro
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.
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Cell Line:Primary mouse cardiomyocytes treated with high glucose (30 mmol/L)
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Concentration:2.5, 5 μM
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Incubation Time:24 h
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Result:Inhibited NLRP3 and caspase-1 at 2.5 and 5 µM.
Increased the p-AMPK.
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Cell Line:Cardiac microvascular endothelial cells isolated from 1- to 4-day-old SD rats
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Concentration:1, 3 μM
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Incubation Time:12 h
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Result:Suppressed reactive oxygen species (ROS) and the vascular adhesion molecule ICAM-1.
Suppressed transcriptional factor Egr-1 expression.
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Cell Line:Human dental pulp cell
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Concentration:2.5, 5 μM
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Incubation Time:24 h
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Result:Suppressed c-Jun and c-Fos expression
Suppressed nuclear p65 protein accumulation
In Vivo
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
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