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Losartan Carboxylic Acid

Name: Losartan Carboxylic Acid
Brand: TargetMol
SKU: T3461
Price: 29 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3461Cas No. 124750-92-1

Alias EXP-3174, E-3174

Losartan Carboxylic Acid (E-3174), a potent AT1 antagonist (Kis: 0.57 nM, rat; 0.67 nM, human), produces a depressor response and vasodilatation. As a metabolite of losartan, it is more potent than losartan in blocking angiotensin II-induced responses in vascular smooth muscle cells.

Losartan Carboxylic Acid

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Purity: 99.28%

Catalog No. T3461Alias EXP-3174, E-3174Cas No. 124750-92-1

Pack Size	Price	USA Warehouse	Global Warehouse
10 mg	$43	In Stock	In Stock
25 mg	$88	In Stock	In Stock
50 mg	$158	In Stock	In Stock
100 mg	$236	In Stock	-
200 mg	$346	In Stock	-
1 mL x 10 mM (in DMSO)	$29	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.28%

Appearance:Solid

Color:White

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Product Introduction

Losartan Carboxylic Acid AI Summary

Losartan Carboxylic Acid exhibits potent bioactivity as an angiotensin II receptor type 1 (AT1) antagonist. It shows high in vitro binding affinity for the AT1 receptor in various systems, including rabbit aorta membranes with an IC50 of 2.8 nM, rat adrenal cortical membranes with Ki values ranging from 6.8 nM to 37 nM, and rat liver AT1 receptor with an IC50 of 14 nM. In vivo studies indicate that Losartan Carboxylic Acid effectively inhibits angiotensin II-induced pressor responses in normotensive and renal hypertensive rats, providing significant antihypertensive effects with oral and intravenous ED30 values of 0.66 mg/kg and 0.038 mg/kg, respectively. Additionally, the compound demonstrates prolonged durations of action exceeding 29 hours at certain doses. It also exhibits a high plasma protein binding rate (~99.5%) and displays varied metabolic and pharmacokinetic characteristics influenced by genetic polymorphisms and gender differences. While its primary bioactivity is angiotensin II receptor antagonism, Losartan Carboxylic Acid has also shown some antiviral activity against SARS-CoV-2, though with limited efficacy, and moderate antioxidant properties..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Losartan Carboxylic Acid (E-3174), a potent AT1 antagonist (Kis: 0.57 nM, rat; 0.67 nM, human), produces a depressor response and vasodilatation. As a metabolite of losartan, it is more potent than losartan in blocking angiotensin II-induced responses in vascular smooth muscle cells.
Synonyms	EXP-3174, E-3174

Chemical Properties

Molecular Weight	436.89
Formula	C₂₂H₂₁ClN₆O₂
Cas No.	124750-92-1
Smiles	C(N1C(CCCC)=NC(Cl)=C1C(O)=O)C2=CC=C(C=C2)C3=C(C=CC=C3)C=4NN=NN4
Relative Density.	1.41 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 70 mg/mL (160.22 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.58 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2889 mL	11.4445 mL	22.8891 mL	114.4453 mL
5 mM	0.4578 mL	2.2889 mL	4.5778 mL	22.8891 mL
10 mM	0.2289 mL	1.1445 mL	2.2889 mL	11.4445 mL
20 mM	0.1144 mL	0.5722 mL	1.1445 mL	5.7223 mL
50 mM	0.0458 mL	0.2289 mL	0.4578 mL	2.2889 mL
100 mM	0.0229 mL	0.1144 mL	0.2289 mL	1.1445 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc