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Losartan Carboxylic Acid

CAS No. : 124750-92-1

MCE 站：Losartan Carboxylic Acid

产品活性：Losartan Carboxylic Acid (E-3174) 是 Losartan 的活性羧酸代谢产物，是血管紧张素 Ⅱ 受体 1 型 (AT1) 拮抗剂。对大鼠 AT1B/AT1A 和人 AT1 的 K_i 值分别为 0.97、0.57、0.67 nM。Losartan Carboxylic Acid 阻断血管紧张素II诱导的血管平滑肌细胞 (VSMC) 反应。Losartan Carboxylic Acid 升高血浆肾素活性，降低平均动脉压。

研究领域：GPCR/G Protein

作用靶点：Angiotensin Receptor

In Vitro: The specific binding of [125I]-angiotensin II to VSMC is inhibited by Losartan Carboxylic Acid (E-3174) with an IC₅₀ of 1.1 nM. Losartan Carboxylic Acid abolishes the angiotensin II-induced formation of inositolphosphates in VSMC. Losartan Carboxylic Acid inhibits the angiotensin II-induced elevation of intracellular cytosolic Ca2+ concentration with an IC₅₀ of 5 nM. Losartan Carboxylic Acid is more effective than losartan in blocking the angiotensin II-induced increase in Egr-1 mRNA. Losartan Carboxylic Acid inhibits the angiotensin II-induced cell protein synthesis with an IC₅₀ of 3 nM.

In Vivo: Losartan Carboxylic Acid (E-3174) (0.1 mg/kg; i.v. followed by 0.02 mg/kg/h for 5.5 h) induces a similar level of inhibition (87±4%) of the pressor responses to angiotensin I.
Intravenous Losartan Carboxylic Acid (0.1 mg/kg+0.01 mg/kg/min) is infused in anesthetized dogs with recent (8.1±0.4 days) anterior myocardial infarction. Electrolytic injury of the left circumflex coronary artery to induce thrombotic occlusion and posterolateral ischemia is initiated 1 h after the start of treatment.

相关产品：GPCR/G Protein Compound Library  |  Neurotransmitter Receptor Compound Library  |  Anti-Cardiovascular Disease Compound Library  |  Bioactive Compound Library Plus  |  Angiotensin II human  |  Losartan  |  PD 123319 ditrifluoroacetate  |  Telmisartan  |  A 779  |  AVE 0991  |  Valsartan  |  Tranilast  |  Olmesartan  |  Olodanrigan  |  Candesartan  |  Irbesartan  |  CGP-42112  |  C-Type Natriuretic Peptide (CNP) (1-22), human  |  Sparsentan  |  Fimasartan  |  YS-49  |  Angiotensin II 5-valine  |  AT2 receptor agonist C21  |  Eprosartan mesylate  |  Angiotensin II (3-8), human TFA  |  H-Val-Pro-Pro-OH TFA  |  TRV-120027 TFA  |  Azilsartan (medoxomil)  |  Tasosartan

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