[CAS NO. 124750-92-1] Losartan Carboxylic Acid (EXP-3174)

Name: Losartan Carboxylic Acid (EXP-3174)
Brand: Arctom Scientific
SKU: SLK-S5980

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [124750-92-1]

Store

Catalog

SLK-S5980

Brand

Selleck

CAS

124750-92-1

DESCRIPTION [124750-92-1]

Overview

MDL	MFCD00871928
Molecular Weight	436.89
Molecular Formula	C22H21ClN6O2
SMILES	C(N1C(CCCC)=NC(Cl)=C1C(O)=O)C2=CC=C(C=C2)C3=C(C=CC=C3)C=4NN=NN4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume 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
50 mM	0.0458 mL	0.2289 mL	0.4578 mL

Description

Losartan Carboxylic Acid (E-3174, EXP-3174), an active carboxylic acid metabolite of Losartan, is a non-peptide antagonist. Losartan Carboxylic Acid inhibits the specific binding of [125I]-angiotensin II to VSMC with IC50 of 1.1 nM.

Targets

binding of [125I]-angiotensin II to VSMC ^[1]
(Cell-free assay)

1.1 nM

In vitro

In vitro, losartan competes with the binding of angiotensin II to AT1 receptors; the concentration that inhibits 50% of the binding of angiotensin II (IC50) is 20 nmol/L. Losartan increases AMPK phosphorylation in a time- and dose-dependent manner in VSMCs. It also increases ACC phosphorylation, a major downstream target protein in the AMPK signaling cascade, and LKB1 phosphorylation, which is an upstream kinase of AMPK. Losartan increases p53 and p21 expression in a time-dependent manner, whereas the levels of p27 are not changed. Losartan suppresses Ang II-induced Rb phosphorylation, as well as cyclin D and cyclin E expression which are required for cell cycle progression. The mechanism of growth suppression by losartan is therefore G0/G1 cell cycle arrest which is reversed by AMPK inhibition, such as compound C or AMPK siRNA, but not by apoptosis.

References

[1] A Sachinidis, et al. J Hypertens. 1993 Feb;11(2):155-62.
[2] Burnier M. Circulation. 2001, 103(6):904-12.
[3] Jung Eun Kim, et al. Korean J Physiol Pharmacol. 2010, 14(5): 299–304.
[4] Yao EH, et al. Hypertens Res. 2007, 30(11):1119-28.

Synonyms

1H-Imidazole-5-carboxylic acid, 2-butyl-4-chloro-1-[[2′-(2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-

1H-Imidazole-5-carboxylic acid, 2-butyl-4-chloro-1-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-

2-Butyl-4-chloro-1-[[2′-(2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic acid

EXP 3174

E 3174

Losartan carboxylic acid

2-Butyl-5-chloro-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazole-4-carboxylic acid