1. GPCR/G Protein
  2. Endothelin Receptor
  3. ABT-546

ABT-546 (Synonyms: A-216546)

Cat. No.: HY-135283
Handling Instructions

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. 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 with IC50 of 0.59 nM and 3 nM, respectively.

For research use only. We do not sell to patients.

ABT-546 Chemical Structure

ABT-546 Chemical Structure

CAS No. : 212481-66-8

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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. 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 with IC50 of 0.59 nM and 3 nM, respectively[1].

IC50 & Target[1]

ETA

0.46 nM (Ki)

In Vitro

ABT-546 (A-216546) effectively inhibits specific I endothelin-1 binding to endothelin ETA receptor in membranes prepared from rat pituitary MMQ cells with an IC50 value of 0.56 nM. ABT-546 is much less effective in inhibiting specific [125I]endothelin-3 binding to endothelin ETB rceptor in membranes prepared from porcine cerebellum with an IC50 value of 16,700 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 with an IC50 value of 0.49 nM, but is less effective in inhibiting specific [125I]endothelin-3 binding to endothelin ETB receptor with an IC50 value of 15,400 nM[1].
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[1].

In Vivo

ABT-546 (A-216546; 0-100 mg/kg; oral administration; for 1 hour or 4 hours; male Sprague-Dawley rats) treatment dose-dependently blocks endothelin-1-induced pressor response in conscious rats[1].

Animal Model: Male Sprague-Dawley rats (250-350 g) induced with endothelin-1[1]
Dosage: 0.1 mg/kg, 1 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
Administration: Oral administration; for 1 hour or 4 hours
Result: Exhibited a dose-dependent inhibition of the peak pressor response to endothelin-1, and statistically significant inhibition was achieved at doses of 3 to 100 mg/kg.
Molecular Weight

532.71

Formula

C₃₀H₄₈N₂O₆

CAS No.

212481-66-8

SMILES

O=C([[email protected]]1[[email protected]](CC(C)(C)CCC)N(CC(N(CCCC)CCCC)=O)C[[email protected]@H]1C2=CC(OC)=C(OCO3)C3=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.

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Keywords:

ABT-546A-216546ABT546ABT 546A216546A 216546Endothelin ReceptorETAendothelin-1-mediatedphosphatidylinositolarachidonicacidreleasevasoconstrictionpressorInhibitorinhibitorinhibit

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ABT-546
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