Irbesartan

製品コードS1507 バッチS150702

化学情報

	Synonyms	BMS-186295, SR-47436	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₅H₂₈N₆O
	分子量	428.53	CAS No.	138402-11-6
Solubility (25°C)*	体外	DMSO	1 mg/mL warmed with 50ºC water bath (2.33 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	Irbesartan is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM.
in vitro	Irbesartan competes with angiotensin II (AII) for binding at the AT1 receptor subtype and antagonizes AII-induced contraction in rabbit aorta ring with IC50 of 4 nM. Irbesartan has no affinity for AT2 receptors. ^[1] Irbesartan (10 μM) blocks angiotensin II induced increase in α_v, β₁, β₃, and β₅ integrins, osteopontin, and α-actinin mRNA and protein levels in rat cardiac fibroblasts, leading to the decrease of cell attachment to extracellular matrix (ECM) proteins. ^[2] Irbesartan treatment markedly induces the expression of the adipogenic marker gene adipose protein 2 (aP2) in 3T3-L1 cells in a concentration-dependent manner with EC50 of 3.5 μM and 3.3-fold induction at the concentration of 10 μM. Irbesartan (10 μM) markedly induces transcriptional activity of the peroxisome proliferator–activated receptor-γ (PPARγ) by 3.4-fold independent of its AT1 receptor blocking action. ^[3] Pretreatment with Irbesartan (~10 μM) decreases angiotensin II-induced apoptosis in rat vascular smooth muscle cells by blocking angiotensin II internalization in a concentrationdependent manner. ^[4]
in vivo	Oral administration of Irbesartan (1 mg/kg) reduces angiotensin II (AII)-induced hypertension, equipotent with losartan in conscious normotensive rats, markedly more active than losartan (10 mg/kg) in normotensive cynomolgus monkeys. ^[1] Administration of Irbesartan (7 mg/kg/day) significantly prevents skeletal muscle apoptosis and muscle atrophy in rats with monocrotaline-induced congestive heart failure (CHF), which is involved with the decrease of TNFα level and attributed to AT1 receptor blocking. ^[5]
特徴	Irbesartan is a longer acting AT1 receptor antagonist relative to losartan and valsartan.

プロトコル(参考用のみ)

キナーゼアッセイ	Angiotensin II Binding Study on Rat Liver Membranes
キナーゼアッセイ	The plasma membranes of livers are purified from male Sprague-Dawley rats, and diluted in the incubation buffer (20 mM Tris-HCI, 10 mM MgCI₂, 2 g/L RSA, 145 mg/L bacitracin, pH 7.5). Aliquots of membrane suspension (20-330 μg protein/assay) are incubated for 1 hour at 25 °C with [¹²⁵I]angiotensin II (AII) and various concentrations of Irbesartan in 200 μL of incubation buffer. The incubation is stopped by rapid filtration through a Whatman GF/B filter followed by three consecutive washing sin 5 mL of cold incubation buffer (the GF/B filters are preincubated for 1 hour in the incubation buffer). The radioactivity bound to the filter is counted in a γ counter. Specific binding is defined as the difference between total binding and the binding in the presence of 1 μM unlabeled angiotensin II (AII). The concentration of Irbesartan producing 50% inhibition (IC50) of radioligand binding is determined from competition curve.
動物実験	動物モデル	Male Sprague-Dawley rats and female cynomolgus monkeys (Macaca fascicularis) injected (iv) with angiotensin II (AII)
	投薬量	1 mg/kg
	投与方法	Oral gavage

参考

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カスタマーフィードバック

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

: , , Antiviral Res, 2015, 120:140-6.

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：

Organic anion transporting polypeptide 2B1 (OATP2B1), an expanded substrate profile, does it align with OATP2B1's hypothesized function? [ Xenobiotica, 2020, 10.1080/00498254.2020.1745318]	PubMed: 32189541
Irbesartan Ameliorates Lipid Deposition by Enhancing Autophagy via PKC/AMPK/ULK1 Axis in Free Fatty Acid Induced Hepatocytes. [ Front Physiol, 2019, 10:681]	PubMed: 31191364
Irbesartan, an FDA approved drug for hypertension and diabetic nephropathy, is a potent inhibitor for hepatitis B virus entry by disturbing Na+-dependent taurocholate cotransporting polypeptide activity [Wang XJ, et al. Antiviral Res, 2015, 120:140-6]	PubMed: 26086883
Suppression of adrenal barrestin7-dependent aldosteroneproduction by ARBs: head-to-head comparison [Dabul S, et al. Sci Rep, 2015, 5:8116]	PubMed: 25631300
Lysophosphatidic acid enhances survival of human CD34(+) cells in ischemic conditions. [ Sci Rep, 2015, 5:16406]	PubMed: 26553339

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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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