Home GPCR & G Protein Endothelin Receptor antagonist BQ-123 For research use only.

BQ-123

BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.

BQ-123 Chemical Structure

BQ-123 Chemical Structure

CAS No. 136553-81-6

Purity & Quality Control

BQ-123 Related Products

Signaling Pathway

Endothelin Receptor Signaling Pathways

Endothelin Receptor Signaling Pathway

Biological Activity

Description BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.
Targets
Endothelin A receptor [1]
(Cell-free assay)
7.3 nM
In vitro
In vitro In porcine aortic vascular smooth muscle cells, BQ-123 selectively inhibits ETA-mediated contraction. [1] In rat vascular smooth muscle cells, BQ-123 inhibits endothelin-1-induced phosphoinositide breakdown and DNA synthesis. [2]
In Vivo
In vivo In rats, BQ-123 (1 mg/kg, i.v.) ameliorates myocardial ischemic-reperfusion injury. [3] In rats with pentylenetetrazole (PTZ)-induced tonic-clonic seizures, BQ-123 (3 mg/kg, i.v.) potently impedes the formation and spread of seizure. [4] In pregnant C57BL/6 mice, BQ-123 (6.7 mg/kg, i.p.) prevents LPS-induced preterm birth in mice via the induction of uterine and placental IL-10. [5]
Animal Research Animal Models Male Wistar rats
Dosages 1 mg/kg
Administration i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04449198 Recruiting
Type 1 Diabetes
Augusta University
 October 14 2020 Early Phase 1
NCT00745693 Completed
Coronary Disease
University of Edinburgh|Umeå University
 March 2008 Not Applicable

Chemical Information & Solubility

Molecular Weight 610.7 Formula

C31H42N6O7
CAS No. 136553-81-6 SDF Download BQ-123 SDF
Smiles CC(C)CC1C(=O)NC(C(=O)NC(C(=O)N2CCCC2C(=O)NC(C(=O)N1)C(C)C)CC(=O)O)CC3=CNC4=CC=CC=C43
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (163.74 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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