MCE products for research use only. We do not sell to patients.

Teneligliptin

MCE China：Teneligliptin

Brand：MedChemExpress (MCE)

Cat. No.HY-14806

CAS：760937-92-6

Synonyms：MP-513

Purity：99.04%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

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].

In Vivo：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

IC50 & Target：DPP-4

Hot selling product：Suc-Ala-Leu-Pro-Phe-pNA  | 187-1, N-WASP inhibitor  | Caftaric acid  | Clonidine (hydrochloride)  | Lenvatinib-d4  | N-3-Oxo-tetradecanoyl-L-homoserine lactone  | BTX161  | Pelargonidin (chloride)  | 2-Iminothiolane (hydrochloride)  | Adenosine dialdehyde

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides

References：

[1]. Yoshida T, et al. Discovery and preclinical profile of teneligliptin (3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine): a highly potent, selective, long-lasting and orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Bioorg Med Chem. 2012 Oct 1;20(19):5705-19.  [Content Brief]

[2]. Guo D, et al. Beneficial effects of combination therapy of canagliflozin and teneligliptin on diabetic polyneuropathy and β-cell volume density in spontaneously type 2 diabetic Goto-Kakizaki rats. Metabolism. 2020 Jun;107:154232.  [Content Brief]

[3]. Zhang GL, et al. Teneligliptin mitigates diabetic cardiomyopathy by inhibiting activation of the NLRP3 inflammasome. World J Diabetes. 2024 Apr 15;15(4):724-734.  [Content Brief]

[4]. Fukuda-Tsuru S, et al. The novel dipeptidyl peptidase-4 inhibitor teneligliptin prevents high-fat diet-induced obesity accompanied with increased energy expenditure in mice. Eur J Pharmacol. 2014 Jan 15;723:207-15.  [Content Brief]

[5]. Zhang Z, et al. Teneligliptin protects against hypoxia/reoxygenation-induced endothelial cell injury. Biomed Pharmacother. 2019 Jan;109:468-474.  [Content Brief]

[6]. Peng W, et al. Teneligliptin prevents doxorubicin-induced inflammation and apoptosis in H9c2 cells. Arch Biochem Biophys. 2020 Apr 15;683:108238.  [Content Brief]

[7]. Liu X, et al. Teneligliptin inhibits lipopolysaccharide-induced cytotoxicity and inflammation in dental pulp cells. Int Immunopharmacol. 2019 Aug;73:57-63.  [Content Brief]

[8]. Elumalai S, et al. High glucose-induced PRDX3 acetylation contributes to glucotoxicity in pancreatic β-cells: Prevention by Teneligliptin. Free Radic Biol Med. 2020 Nov 20;160:618-629.  [Content Brief]