Home Proteases DPP inhibitor Teneligliptin hydrobromide For research use only.

Teneligliptin hydrobromide

Synonyms: Teneligliptin hydrobromide anhydrous

Teneligliptin (Teneligliptin hydrobromide anhydrous) 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.

Teneligliptin hydrobromide Chemical Structure

Teneligliptin hydrobromide Chemical Structure

CAS No. 906093-29-6

Purity & Quality Control

Teneligliptin hydrobromide Related Products

Signaling Pathway

DPP Signaling Pathways

DPP Signaling Pathway

Biological Activity

Description Teneligliptin (Teneligliptin hydrobromide anhydrous) 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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models C57BL6/J mice
Dosages 60 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 628.86 Formula

C22H30N6OS.5/2HBr
CAS No. 906093-29-6 SDF Download Teneligliptin hydrobromide SDF
Smiles CC1=NN(C(=C1)N2CCN(CC2)C3CC(NC3)C(=O)N4CCSC4)C5=CC=CC=C5.CC1=NN(C(=C1)N2CCN(CC2)C3CC(NC3)C(=O)N4CCSC4)C5=CC=CC=C5.Br.Br.Br.Br.Br
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (159.01 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : 17 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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