2. GPCR/G Protein
  3. Endothelin Receptor
  4. 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. 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.

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ABT-546 Chemical Structure

ABT-546 Chemical Structure

CAS No. : 212481-66-8

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ABT-546 Related Antibodies

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1 Publications Citing Use of MCE ABT-546

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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)

Cellular Effect
Cell Line Type Value Description References
Pituitary gland cell IC50
0.56 nM
Compound: 10a
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
Binding affinity for endothelin A receptor by measuring its ability to displace [125I]ET1 from prolactin secreting rat pituitary cells(MMQ)
[PMID: 9703472]
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].

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

ABT-546 Related Antibodies
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].

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

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.
SMILES

O=C([C@H]1[C@H](CC(C)(C)CCC)N(CC(N(CCCC)CCCC)=O)C[C@@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.
Purity & Documentation
References
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ABT-546 Related Classifications

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Help & FAQs
  • 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.

Keywords:

ABT-546212481-66-8A-216546ABT546ABT 546A216546A 216546Endothelin ReceptorETAendothelin-1-mediatedphosphatidylinositolarachidonicacidreleasevasoconstrictionpressorInhibitorinhibitorinhibit

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