1. GPCR/G Protein
  2. Angiotensin Receptor
  3. Losartan Carboxylic Acid

Losartan Carboxylic Acid (Synonyms: E-3174; EXP-3174)

Cat. No.: HY-12765 Purity: 98.00%
Handling Instructions

Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure.

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Losartan Carboxylic Acid Chemical Structure

Losartan Carboxylic Acid Chemical Structure

CAS No. : 124750-92-1

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10 mM * 1  mL in DMSO USD 77 In-stock
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10 mg USD 135 In-stock
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50 mg USD 450 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure[1][2][3][4].

IC50 & Target

Angiotensin II receptor type 1[1]

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[1].

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[3].
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[4].

Animal Model: Mongrel dogs of either sex, weighing 15-25 kg[3]
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%.
Molecular Weight

436.89

Formula

C₂₂H₂₁ClN₆O₂

CAS No.

124750-92-1

SMILES

O=C(C1=C(Cl)N=C(CCCC)N1CC2=CC=C(C3=CC=CC=C3C4=NNN=N4)C=C2)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 250 mg/mL (572.23 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2889 mL 11.4445 mL 22.8891 mL
5 mM 0.4578 mL 2.2889 mL 4.5778 mL
10 mM 0.2289 mL 1.1445 mL 2.2889 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.76 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.76 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

Losartan Carboxylic AcidE-3174EXP-3174E3174E 3174EXP3174EXP 3174Angiotensin Receptormetabolitevascularsmoothmusclecellsangiotensin IIanteriormyocardialinfarctionpressorresponsesInhibitorinhibitorinhibit

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Product Name:
Losartan Carboxylic Acid
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HY-12765
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