Losartan Carboxylic Acid

CAS No. 124750-92-1

Losartan Carboxylic Acid( EXP-3174 | EXP 3174 | Losartan Carboxylic Acid )

Catalog No. M17904 CAS No. 124750-92-1

EXP-3174 is a potent AT1 antagonist (Kis: 0.57 nM, rat; 0.67 nM, human), producing a depressor response and vasodilatation.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
5MG 39 In Stock
10MG 65 In Stock
25MG 132 In Stock
50MG 237 In Stock
100MG 354 In Stock
200MG 518 In Stock
500MG Get Quote In Stock
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Biological Information

  • Product Name
    Losartan Carboxylic Acid
  • Note
    Research use only, not for human use.
  • Brief Description
    EXP-3174 is a potent AT1 antagonist (Kis: 0.57 nM, rat; 0.67 nM, human), producing a depressor response and vasodilatation.
  • Description
    EXP-3174, also known as Losartan Carboxylic Acid, is a physiologically active metabolite of losartan, produced by cytochrome P450 isoforms in the liver. Like the parent compound, EXP-3174 is a potent AT1 antagonist (Kis = 0.57 and 0.67 nM for rat and human forms, respectively), producing a depressor response and vasodilatation. When administered intravenously, losartan carboxylic acid is more potent and has a longer duration of action than losartan. However, the metabolite has very low oral bioavailability.(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.
  • 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. Animal Model:Mongrel dogs of either sex, weighing 15-25 kg Dosage:0.1 mg/kg (followed by 0.02 mg/kg/h)Administration:i.v. for 5.5 hours Result:The pressor response was reduced by 87±4%.
  • Synonyms
    EXP-3174 | EXP 3174 | Losartan Carboxylic Acid
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    AT1 receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    124750-92-1
  • Formula Weight
    436.9
  • Molecular Formula
    C22H21ClN6O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : ≥ 250 mg/mL (572.23 mM)
  • SMILES
    c1(n(c(c(n1)Cl)C(=O)O)Cc1ccc(cc1)c1c(cccc1)c1n[nH]nn1)CCCC
  • Chemical Name
    1-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-4-chloro-1H-imidazole-5-carboxylic acid

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Choi JS, Choi JS, Choi DH. Effects of licochalcon A on the pharmacokinetics of losartan and its active metabolite, EXP-3174, in rats. Pharmazie. 2013 Nov;68(11):882-8.
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