Telmisartan

製品コードS1738 バッチS173802

化学情報

	Synonyms	BIBR 277	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₃₃H₃₀N₄O₂
	分子量	514.62	CAS No.	144701-48-4
Solubility (25°C)*	体外	DMSO	13 mg/mL warmed with 50ºC water bath (25.26 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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	Telmisartan (BIBR 277) is an angiotensin II receptor antagonist (ARB) used in the management of hypertension.
in vitro	Telmisartan functions as a moderately potent (EC50=4.5 μM), selective PPARγ partial agonist, activating the receptor to 25% to 30% of the maximum level achieved by the full agonists pioglitazone and rosiglitazone. Telmisartan induces adipocyte differentiation of 3T3-L1 cells. Telmisartan causes a 60% to 70% decrease in the expression of ACC2 in murine muscle myotubes. ^[1] Telmisartan, but not candesartan, another ARB, downregulates RAGE mRNA levels in a dose-dependent manner. Telmisartan decreases basal as well as AGE-induced RAGE protein expression in Hep3B cells. Telmisartan dose-dependently inhibits AGE-induced ROS generation and subsequent CRP gene and protein induction in Hep3B cells. ^[2] Telmisartan effectively facilitates differentiation of 3T3-L1 preadipocytes. Telmisartan causes a dose-dependent increase in mRNA levels for PPARgamma target genes such as aP2 and adiponectin in both differentiating adipocytes and fully differentiated adipocytes. Telmisartan attenuates 11beta-hydroxysteroid dehydrogenase type 1 mRNA level in differentiated adipocytes. ^[3]
in vivo	Telmisartan promotes increases in caloric expenditure and protects against dietary-induced weight gain in rats fed with a high-fat, high-carbohydrate diet. Telmisartan reduces the accumulation of visceral fat and decreases adipocyte size to a much greater extent than valsartan and is also associated with a significant reduction in hepatic triglyceride levels in rats fed with a high-fat, high-carbohydrate diet. ^[4]

プロトコル(参考用のみ)

参考

[4] Sugimoto K et al. Hypertension, 2006, 47(5), 1003-1009.

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カスタマーフィードバック

: , , Sci Rep, 2015, 5:8116.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Telmisartan inhibits bladder smooth muscle fibrosis in neurogenic bladder rats [ Exp Ther Med, 2022, 23(3):216]	PubMed: 35126719
Trypsin-Mediated Sensitization to Ferroptosis Increases the Severity of Pancreatitis in Mice [ Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X]	PubMed: 34562639
Inhibiting STAT5 significantly attenuated Ang II-induced cardiac dysfunction and inflammation [ Eur J Pharmacol, 2021, S0014-2999(21)00845-1]	PubMed: 34919891
Actinomycin D and Telmisartan Combination Targets Lung Cancer Stem Cells Through the Wnt/Beta Catenin Pathway. [ Sci Rep, 2019, 9(1):18177]	PubMed: 31796785
Brain Renin-Angiotensin System Blockade Attenuates Methamphetamine-Induced Hyperlocomotion and Neurotoxicity [Jiang L, et al. Neurotherapeutics, 2018, 15(2):500-510]	PubMed: 29464572
A network integration approach for drug-target interaction prediction and computational drug repositioning from heterogeneous information. [ Nat Commun, 2017, 8(1):573]	PubMed: 28924171
Suppression of adrenal barrestin1-dependent aldosteroneproduction by ARBs: head-to-head comparison [Dabul S, et al. Sci Rep, 2015, 5:8116]	PubMed: 25631300

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。