Teneligliptin hydrobromide

Catalog No.S4636 Batch:S463602

Technical Data

Formula	C₂₂H₃₀N₆OS.5/2HBr
Molecular Weight	628.86	CAS No.	906093-29-6
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (159.01 mM)
		Water	100 mg/mL (159.01 mM)
		Ethanol	6 mg/mL (9.54 mM)
* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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 (from reference)

Cell Assay:^{^[4]}	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.
Animal Study:^{^[2]}	Animal Models C57BL6/J mice Dosages 60 mg/kg Administration p.o.

Cell Assay:^{^[4]}

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.

Animal Study:^{^[2]}

Animal Models
C57BL6/J mice
Dosages
60 mg/kg
Administration
p.o.

References

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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