Losartan

製品コードS5067 バッチS506702

印刷

化学情報

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

82 mg/mL (193.89 mM)

Ethanol

82 mg/mL (193.89 mM)

Water

Insoluble

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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	6.000mg/ml (14.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 120 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	6.000mg/ml (14.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 120 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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]. This compound 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. It increases p53 and p21 expression in a time-dependent manner, whereas the levels of p27 are not changed. This chemical 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 this compound 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, this compound is 10 to 20 times more potent than losartan and has a longer duration of action than this chemical. However, the oral bioavailability of EXP 3174 is very low. This compound 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 this compound 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

参考

https://pubmed.ncbi.nlm.nih.gov/11171802/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2997415/
https://pubmed.ncbi.nlm.nih.gov/18250561/

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：

Reposition of lenalidomide as a radiation protector based on LINCS gene expression signatures and its preclinical validation [ Sci Rep, 2025, 15(1):12955]	PubMed: 40234645
Determining sex differences in aortic valve myofibroblast responses to drug combinations identified using a digital medicine platform [ Sci Adv, 2025, 11(23):eadu2695]	PubMed: 40479052
Downregulation of salusins alleviates hypertrophic cardiomyopathy via attenuating oxidative stress and autophagy [ Eur J Med Res, 2024, 29(1):109]	PubMed: 38336819
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
Antiviral activity evaluation of pharmaceutical drugs, newly synthesized compounds and fragments against SARS-CoV-2 in vitro [ UNIVERSITY OF PÉCS, 2023, ]	PubMed: None
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

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。