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 |
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10MG | 65 | In Stock |
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25MG | 132 | In Stock |
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50MG | 237 | In Stock |
|
100MG | 354 | In Stock |
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200MG | 518 | In Stock |
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500MG | Get Quote | In Stock |
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1G | Get Quote | In Stock |
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Biological Information
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Product NameLosartan Carboxylic Acid
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NoteResearch use only, not for human use.
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Brief DescriptionEXP-3174 is a potent AT1 antagonist (Kis: 0.57 nM, rat; 0.67 nM, human), producing a depressor response and vasodilatation.
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DescriptionEXP-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.
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In VitroThe 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.
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In VivoLosartan 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%.
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SynonymsEXP-3174 | EXP 3174 | Losartan Carboxylic Acid
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PathwayOthers
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TargetOther Targets
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RecptorAT1 receptor
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Research Area——
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Indication——
Chemical Information
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CAS Number124750-92-1
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Formula Weight436.9
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Molecular FormulaC22H21ClN6O2
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : ≥ 250 mg/mL (572.23 mM)
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SMILESc1(n(c(c(n1)Cl)C(=O)O)Cc1ccc(cc1)c1c(cccc1)c1n[nH]nn1)CCCC
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Chemical Name1-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-4-chloro-1H-imidazole-5-carboxylic acid
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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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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