Teneligliptin hydrobromide

製品コードS4636 バッチS463601

印刷

化学情報

Synonyms

Teneligliptin hydrobromide anhydrous

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₂H₃₀N₆OS.5/2HBr

分子量

628.86

CAS No.

906093-29-6

Solubility (25°C)*

体外

DMSO

100 mg/mL (159.01 mM)

Water

100 mg/mL (159.01 mM)

Ethanol

17 mg/mL (27.03 mM)

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Teneligliptin (Teneligliptin hydrobromide anhydrous) は、新規の強力で持続性のあるdipeptidyl peptidase-4阻害剤です。in vitroでヒト血漿、ラット血漿、およびヒト組換えDPP-4を競合的に阻害し、IC50値は約1 nMでした。
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.
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. It is found that this compound attenuates lipogenesis in the liver by activating AMPK and downregulating the expression of genes involved in lipogenesis.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Human umbilical vein endothelial primary cells (HUVECs)
	濃度	0.1, 1.0 or 3.0 µmol/L
	反応時間	21 days
	実験の流れ	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.
動物実験	動物モデル	C57BL6/J mice
	投薬量	60 mg/kg
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/23671395/
https://pubmed.ncbi.nlm.nih.gov/26264980/
https://pubmed.ncbi.nlm.nih.gov/26670228/

https://pubmed.ncbi.nlm.nih.gov/27530507/
https://pubmed.ncbi.nlm.nih.gov/23022337/

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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