L-162782 

L-162782 is a high affinity AT₁ receptor ligand for rat and human wild-type AT₁ with IC₅₀ values of 28.5 and 24.6 nM, respectively. L-162782 acts as a partial agonist (EC₅₀ ≈ 30 nM) and insurmountable antagonist (IC₅₀ = 6.5 μM) on wild-type rat AT₁ receptors in COS-7 cells. L-162782 reduces Angiotensin II (HY-13948)-induced phosphatidylinositol turnover. L-162782 can be used for hypertension research^[1].

L-162782 binds with high affinity to wild-type rat and human AT₁ receptors, with binding selectively impaired by the A104V mutation in human AT₁ receptor (20-fold reduction in affinity)^[1].
L-162782 acts as a partial agonist (stimulating phosphatidylinositol turnover to 64% of Angiotensin II response) and antagonist on wild-type rat AT₁ receptors in COS-7 cells^[1].
L-162782 binds with unaltered high affinity to N295D mutant rat AT₁ receptors but has impaired agonistic efficacy (stimulating turnover to 19.4% of Angiotensin II response) and acts as an antagonist with an IC₅₀ of 90-180 nM^[2].

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

576.76

C₃₂H₄₀N₄O₄S

169281-92-9

O=C(OCCCC)NS(=O)(=O)C=1C=CC(=CC1C2=CC=C(C=C2)CN3C4=NC(=CC(=C4N=C3CC)C)C)CC(C)C

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• [1]. Perlman S, et al. Dual agonistic and antagonistic property of nonpeptide angiotensin AT1 ligands: susceptibility to receptor mutations. Mol Pharmacol. 1997;51(2):301-311.  [Content Brief]