Teneligliptin hydrobromide

For research use only.

Catalog No.S4636 Synonyms: Teneligliptin hydrobromide anhydrous

Teneligliptin hydrobromide Chemical Structure

Molecular Weight(MW): 628.86

Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM.

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Biological Activity

Description Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM.
Targets
DPP-4 [1]
()
DPP-9 [1]
1.75 nM 150 nM
In vitro

Chronic teneligliptin treatment at doses between 0.1 and 3.0 µmol/L does not reduce cell viability of HUVECs, but decreases HG-stress markers and increases heme oxygenase-1 (HMOX1) gene expression in HUVEC cells incubated under hyperglycemia. Also, chronic teneligliptin treatment improves proliferative capacities of HUVEC cells and endoplasmic reticulum (ER) function in HUVEC cells exposed to HG. Teneligliptin has antioxidant properties under NG in HUVECs, reducing ROS levels and initiating the transcriptional cascade of the antioxidant genes[4].

In vivo Teneligliptin attenuates body weight gain, fat accumulation, and serum insulin and triglyceride levels in the mouse model of postmenopausal obesity. Also improves glucose intolerance, but dose not affect insulin sensitivity. It attenuates chronic inflammation in perigonadal fat and hepatic steatosis in the mouse model of postmenopausal obesity. Teneligliptin increases locomotor activity in the dark phase and enhanced energy expenditure in postmenopausal obese mice[2]. It is found that this compound attenuates lipogenesis in the liver by activating AMPK and downregulating the expression of genes involved in lipogenesis[3].

Protocol

Cell Research:[4]
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  • Cell lines: Human umbilical vein endothelial primary cells (HUVECs)
  • Concentrations: 0.1, 1.0 or 3.0 µmol/L
  • Incubation Time: 21 days
  • Method: HUVECs are seeded and allowed to attach overnight. Next day cells are exposed to one of three glucose experimental conditions with or without teneligliptin (at 0.1, 1.0 or 3.0 µmol/L) or sitagliptin (at 0.5 µmol/L): continuous normal glucose (NG-5 mmol/L) for 21 days; continuous high glucose (HG-25 mmol/L) for 21 days; and high-metabolic memory (HM-continuous HG for 14 days, followed by NG for the last 7 days). HUVECs are cultured during the 3 weeks changing the media each 48 h and without passaging the cells.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: C57BL6/J mice
  • Dosages: 60 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (159.01 mM)
Water 100 mg/mL (159.01 mM)
Ethanol 17 mg/mL (27.03 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 628.86
Formula

C22H30N6OS.5/2HBr

CAS No. 906093-29-6
Storage powder
in solvent
Synonyms Teneligliptin hydrobromide anhydrous
Smiles CC1=N[N](C2=CC=CC=C2)C(=C1)N3CCN(CC3)C4CNC(C4)C(=O)N5CCSC5

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DPP-4 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID