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ABT-546

ABT-546
ABT-546 (A-216546) is a potent, highly selective, and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [125I]endothelin-1 binding to cloned human endothelin ETA.
Catalog No. T10225Cas No. 212481-66-8
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ABT-546

Catalog No. T10225Cas No. 212481-66-8
ABT-546 (A-216546) is a potent, highly selective, and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [125I]endothelin-1 binding to cloned human endothelin ETA.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
25 mg$1,5206-8 weeks
50 mg$1,9806-8 weeks
100 mg$2,5006-8 weeks
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Product Introduction

Bioactivity
Description
ABT-546 (A-216546) is a potent, highly selective, and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [125I]endothelin-1 binding to cloned human endothelin ETA.
Targets&IC50
ETA:0.46 nM (ki)
In vitro
ABT-546 is >25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis (IC50s: 0.59 nM and 3 nM). ABT-546 effectively inhibits specific I endothelin-1 binding to endothelin ETA receptor in membranes prepared from rat pituitary MMQ cells (IC50: 0.56 nM). In membranes prepared from CHO cells stably transfected with the human endothelin ETA and ETB receptors, ABT-546 again effectively inhibits specific [125I]endothelin-1 binding to endothelin ETA receptor (IC50: 0.49 nM), but is less effective in inhibiting specific [125I]endothelin-3 binding to endothelin ETB receptor (IC50: 15,400 nM). In isolated vessels, ABT-546 inhibits endothelin ETA receptor-mediated endothelin-1-induced vasoconstriction, and endothelin ETB receptor-mediated sarafotoxin 6c-induces vasoconstriction with pA2 of 8.29 and 4.57, respectively.
In vivo
ABT-546 (0-100 mg/kg; p.o.; for 1 hour or 4 hours; male Sprague-Dawley rats) treatment dose-dependently blocks the endothelin-1-induced pressor response in conscious rats.
Animal Research
Animal Model: Male Sprague-Dawley rats (250-350 g) induced with endothelin-1. Dosage: 0.1 mg/kg, 1 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg. Administration: p.o.; for 1 hour or 4 hours
AliasA-216546
Chemical Properties
Molecular Weight532.71
FormulaC30H48N2O6
Cas No.212481-66-8
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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