1. GPCR/G Protein
  2. Angiotensin Receptor
  3. L162389

L162389 is a potent antagonist of angiotensin AT1 receptor with Ki of 28 nM.

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L162389 Chemical Structure

L162389 Chemical Structure

CAS No. : 169281-53-2

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Description

L162389 is a potent antagonist of angiotensin AT1 receptor with Ki of 28 nM.

IC50 & Target

Ki: 28 nM (angiotensin AT1 receptor)[1]

Cellular Effect
Cell Line Type Value Description References
COS-7 IC50
1.5 nM
Compound: 4; L-162,389
Displacement of 125I-[Sar1,Leu8] angiotensin-2 from rat type 1 angiotensin-2 receptor expressed in African green monkey COS7 cells after 24 hrs
Displacement of 125I-[Sar1,Leu8] angiotensin-2 from rat type 1 angiotensin-2 receptor expressed in African green monkey COS7 cells after 24 hrs
[PMID: 26810314]
In Vitro

L-162,389 stimulates phosphatidylinositol turnover, albeit only to a small percentage of the angiotensin response. L-162,389 acts as angiotensin antagonist with IC50 value of 105 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

562.72

Formula

C31H38N4O4S

CAS No.
SMILES

O=C(OCCCC)NS(=O)(C1=CC=C(CCC)C=C1C2=CC=C(CN3C(CC)=NC4=C(C)C=C(C)N=C43)C=C2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
Kinase Assay
[1]

Monoiodinated 125I-[Sar1,Leu8]angiotensin II is prepared by the Iodo-Gen method. One day after transfection and 24 hr before the binding experiments, the transfected cells are transferred to 6-, 12-, or 24-well culture plates, with 0.15-9 × 105 cells/well, with a goal of total binding of 5-10% of the radiolabeled peptide. The cells are washed twice with buffer (25 mM Tris, 5 mM MgCl2, 140 mM NaCl, pH 7.4) before and after the binding. The binding is carried out for 24 hr at 4°C with 50 pm 125I-[Sar1,Leu8]angiotensin II and variable amounts of unlabeled nonpeptide or peptide ligands in 0.5-1 mL of a 25 mM Tris buffer containing 5 mm MgCl2, pH 7.4. The binding data are analyzed by computerized nonlinear regression analysis using InPlot 4.0.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
L162389
Cat. No.:
HY-101618
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