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.
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- CAS No.: 169281-92-9
- 화학식: C32H40N4O4S
- 분자량:576.76
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
All Angiotensin Receptor Isoforms
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Biological Activity
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AT1 Receptor 28.5 (rat) nM (IC50) |
AT1 Receptor 24.6 (huma nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | IC50 |
2.1 nM
Compound: 3; L-162,782
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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
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[PMID: 26810314] |
| COS-7 | IC50 |
2.1 nM
Compound: 7, L-162782
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Displacement of [125I]-[Sar1,Leu8]angiotensin II from human AT1 receptor expressed in african green monkey COS7 cells
Displacement of [125I]-[Sar1,Leu8]angiotensin II from human AT1 receptor expressed in african green monkey COS7 cells
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[PMID: 25699147] |
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.
Chemical Information
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CAS No. 169281-92-9
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분자량 576.76
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화학식 C32H40N4O4S
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SMILES
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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
L-162782 Related Classifications
HY-125094 Related Classifications
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