BQ-123

Catalog No.S7883

For research use only.

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

BQ-123 Chemical Structure

CAS No. 136553-81-6

Selleck's BQ-123 has been cited by 4 Publications

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Purity & Quality Control

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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 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 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]

Protocol (from reference)

Animal Research:[3]
  • Animal Models: Male Wistar rats
  • Dosages: 1 mg/kg
  • Administration: i.v.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 610.7
Formula

C31H42N6O7

CAS No. 136553-81-6
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

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Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04449198 Recruiting Drug: Resveratrol|Other: Placebo Type 1 Diabetes Augusta University October 14 2020 Early Phase 1
NCT00745693 Completed Drug: Endothelin-1|Drug: BQ-123 and BQ-788 Coronary Disease University of Edinburgh|Umeå University March 2008 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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