Name: BQ-123
Brand: Selleck Chemicals
SKU: S7883
Availability: InStock
Rating: 5 (10 reviews)

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other Endothelin Receptor Inhibitors	Zibotentan (ZD4054) Sparsentan (PS-433540, RE-021) Lu-135252 Pearl Extract Carperitide Acetate Atrasentan Aprocitentan

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (163.74 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (8.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (0.82mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight	610.7	Formula	C₃₁H₄₂N₆O₇	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	136553-81-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			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

Mechanism of Action

Targets/IC₅₀/Ki	Endothelin A receptor (Cell-free assay) 7.3 nM
In vitro	In porcine aortic vascular smooth muscle cells, BQ-123 selectively inhibits ETA-mediated contraction. In rat vascular smooth muscle cells, this compound inhibits endothelin-1-induced phosphoinositide breakdown and DNA synthesis.
In vivo	In rats, BQ-123 (1 mg/kg, i.v.) ameliorates myocardial ischemic-reperfusion injury. In rats with pentylenetetrazole (PTZ)-induced tonic-clonic seizures, this compound (3 mg/kg, i.v.) potently impedes the formation and spread of seizure. In pregnant C57BL/6 mice, this chemical (6.7 mg/kg, i.p.) prevents LPS-induced preterm birth in mice via the induction of uterine and placental IL-10.
References	[1] https://pubmed.ncbi.nlm.nih.gov/1282942/ [2] https://pubmed.ncbi.nlm.nih.gov/1318228/ [3] https://pubmed.ncbi.nlm.nih.gov/20888175/ [4] https://pubmed.ncbi.nlm.nih.gov/24449761/ [5] https://pubmed.ncbi.nlm.nih.gov/25230003/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Handling Instructions

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BQ-123 Endothelin Receptor antagonist

Chemical Structure

Molecular Weight: 610.7