Losartan

製品コードS5067 バッチS506701

印刷

化学情報

Chemical Structure Synonyms DuP-753 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C22H23ClN6O
分子量 422.91 CAS No. 114798-26-4
Solubility (25°C)* 体外 DMSO 84 mg/mL (198.62 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Losartan(DuP-753) is a selective, orally administered, nonpeptide blocker of angiotensin II type 1 (AT1) receptor used to treat high blood pressure, diabetic kidney disease, heart failure, and left ventricular enlargement.
in vitro

In vitro, losartan competes with the binding of angiotensin II to AT1 receptors; the concentration that inhibits 50% of the binding of angiotensin II (IC50) is 20 nmol/L[1]. Losartan increases AMPK phosphorylation in a time- and dose-dependent manner in VSMCs. It also increases ACC phosphorylation, a major downstream target protein in the AMPK signaling cascade, and LKB1 phosphorylation, which is an upstream kinase of AMPK. Losartan increases p53 and p21 expression in a time-dependent manner, whereas the levels of p27 are not changed. Losartan suppresses Ang II-induced Rb phosphorylation, as well as cyclin D and cyclin E expression which are required for cell cycle progression. The mechanism of growth suppression by losartan is therefore G0/G1 cell cycle arrest which is reversed by AMPK inhibition, such as compound C or AMPK siRNA, but not by apoptosis[2].
in vivo

Losartan has a major active metabolite, EXP 3174. Administered intravenously, EXP3174 is 10 to 20 times more potent than losartan and has a longer duration of action than losartan. However, the oral bioavailability of EXP 3174 is very low. Losartan has a bioavailability of about 33%, the half-life averages 2 h (6-9 hours), and the rate of protein binding is 98.7% when dosed at 50-100 mg/d[1]. Treatment with losartan ameliorates the loss in the number and function of endothelial progenitor cells (EPCs) in hypertensive rats[3].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 VSMCs
濃度 0, 1, 5, 10 μM
反応時間 48 h
実験の流れ

Cells were treated with Ang II or 15% FBS in the presence or absence of indicated concentration of losartan for 48 hrs. Cell proliferation was determined by the MTT assay.
動物実験 動物モデル 12-week-old male Wistar-Kyoto (WKY) rats and SHR-SP
投薬量 10 mg/kg/day
投与方法 oral

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：

Losartan controls immune checkpoint blocker-induced edema and improves survival in glioblastoma mouse models [ Proc Natl Acad Sci U S A, 2023, 120(6):e2219199120] PubMed: 36724255
Losartan protects human stem cell-derived cardiomyocytes from angiotensin II-induced alcoholic cardiotoxicity [ Cell Death Discov, 2022, 8(1):134] PubMed: 35347130
Effect of Angiotensin-Converting-Enzyme Inhibitor and Angiotensin II Receptor Antagonist Treatment on ACE2 Expression and SARS-CoV-2 Replication in Primary Airway Epithelial Cells [ Front Pharmacol, 2021, 12:765951] PubMed: 34867390
Silencing of central (Pro)renin receptor ameliorates salt-induced renal injury in CKD [ Antioxid Redox Signal, 2020, 10.1089/ars.2019.7840] PubMed: 32757619
Calcilytic NPS2143 promotes proliferation and inhibits apoptosis of spontaneously hypertensive rat vascular smooth muscle cells via activation of the renin-angiotensin system [ Exp Ther Med, 2020, 20(2):818-829] PubMed: 32742325
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
The effects of losartan on cytomegalovirus infection in human trabecular meshwork cells. [ PLoS One, 2019, 14(6):e0218471] PubMed: 31216320
AVE 0991 Attenuates Pyroptosis and Liver Damage after Heatstroke by Inhibiting the ROS-NLRP3 Inflammatory Signalling Pathway. [ Biomed Res Int, 2019, 2019:1806234] PubMed: 31531346
CaSR participates in the regulation of vascular tension in the mesentery of hypertensive rats via the PLC‑IP3/AC‑V/cAMP/RAS pathway [ Mol Med Rep, 2019, 20(5):4433-4448] PubMed: 31485595
Involvement of estrogen receptor and GPER in bisphenol A induced proliferation of vascular smooth muscle cells. [ Toxicol In Vitro, 2019, 56:156-162] PubMed: 30677511

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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