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ABT-546 | ABT-546 : Antagonist of EDNRA
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
EDNRA
  • Ki:0.46 nM
  • IC50:0.59 nM
  • EC50:1.1 nM
Antagonist
may be used up to 10 µM
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
EDNRB: Ki = 13000 nM; Clean GPCR scan CEREP panel of receptors (at 10 µM): closest hits: EDNRB = 56% ...

Potency
Cellular
In Vitro

EDNRA

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/s0014-2999(98)00891-7

In Vivo Validations

Rat
Dose: 5 mg/Kg
Route of delivery: Intravenous
Plasma half life: 1.6 h
Systemic clearance: 1.5 l/h*kg
Volume of Distribution at Steady-State: 0.56 - 3.7 l/kg

DOI Reference: 10.1016/s0014-2999(98)00891-7

Dose: 10 mg/Kg
Route of delivery: Oral
Plasma half life: 2.5 h
Cmax: 1.69 μg/ml
Tmax: 1.3 h
Bioavailability: 47.7%

DOI Reference: 10.1016/s0014-2999(98)00891-7

Dog
Dose: 5 mg/Kg
Route of delivery: Oral
Plasma half life: 3.3 h
Cmax: 1.97 μg/ml
Bioavailability: 19.9 %

DOI Reference: 10.1016/s0014-2999(98)00891-7

Monkey (Cynomolgus)
Dose: 5 mg/Kg
Route of delivery: Oral
Plasma half life: 1 h
Cmax: 1.1 μg/ml
Bioavailability: 18.1 %

DOI Reference: 10.1016/s0014-2999(98)00891-7

Negative Control Compounds

A-545

Chemical Information

Molecular Formula C30H48N2O6
SMILEs CCCCN(CCCC)C(=O)CN1C[C@H](c2cc(OC)c3c(c2)OCO3)[C@@H](C(=O)O)[C@@H]1CC(C)(C)CCC
InChI InChI=1S/C30H48N2O6/c1-7-10-13-31(14-11-8-2)26(33)19-32-18-22(21-15-24(36-6)28-25(16-21)37-20-38-28)27(29(34)35)23(32)17-30(4,5)12-9-3/h15-16,22-23,27H,7-14,17-20H2,1-6H3,(H,34,35)/t22-,23+,27-/m1/s1
Molecular weight 532.35 Da
AlogP 5.5377
HBond acceptors 8
HBond donors 1
Atoms 86

Vendors

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Expert Reviews

by SERP
(on 8 Feb 2022 )
Cellular Use Rating
In Model Organisms
Based on its outstanding (25,000-fold) selectivity for Endothelin A over Endothelin B and excellent selectivity against a panel of 71 GPCR kinases, A-546 is a pharmacologically highly useful tool to study...
by SERP+
(on 14 Oct 2025 )
Cellular Use Rating
In Model Organisms
Generally, this is a highly potent and selective compound in cell assays with minimal off-target effects. It is also in general useful in vivo, though not demonstrating direct target engagement may limit...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria