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BQ-788 sodium salt

Catalog No.GC15916

ET B-receptor antagonist,potent and selective

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BQ-788 sodium salt Chemical Structure

Cas No.: 156161-89-6

Size Price Stock Qty
10mM (in 1mL DMSO)
$428.00
In stock
1mg
$135.00
In stock
5mg
$293.00
In stock
10mg
$419.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

hGH and pCASM cells

Preparation method

The solubility of this compound in DMSO is > 33.2 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

100 μM

Applications

BQ-788 (100 μM) did not increase [Ca2+]i in both hGH and pCASM cells. However, BQ-788 significantly inhibited ET-1-induced increases in [Ca2+]i in both cell lines.

Animal experiment [1]:

Animal models

Rats

Dosage form

1 mg/kg; i.v.

Applications

BQ-788 (1 mg/kg) i.v. administered 5 mins before ET-1 injection completely inhibited the depressor response, correspondingly, causing a rapid onset of apparently enhanced pressor response.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Ishikawa K, Ihara M, Noguchi K, et al. Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proceedings of the National Academy of Sciences, 1994, 91(11): 4892-4896.

Background

BQ-788 is a potent and selective antagonist of endothelin (ET) B-receptor with IC50 value of 1.2nM [1].

In the in vitro assay, BQ-788 prevents ET-1 from binding to ETB receptors in human Girardi heart cells with IC50 value of 1.2nM. The inhibition to ETA receptors is much weaker with IC50 value of 1300nM. BQ-788 also inhibits ET binding to ETB receptors with IC50 values of 0.9nM and 1.2nM in porcine cerebellar membranes and hGH cells, respectively. The inhibition effects are quite poor in pCASM cells and SK-N-MC cells with IC50 values of 280nM and 1300nM, respectively. BQ-788 is specific to ET receptors. It cannot significantly inhibit other peptide hormone receptors at concentration of 10μM. It is found that BQ-788 interacts with ETB receptors competitively in hGH cells. Moreover, the in vivo assay demonstrates that ETB receptors are responsible for ET-1-elicited bronchoconstriction in guinea pigs [1].

References:
[1] Ishikawa K, Ihara M, Noguchi K, et al. Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proceedings of the National Academy of Sciences, 1994, 91(11): 4892-4896.

Chemical Properties

Cas No. 156161-89-6 SDF
Chemical Name sodium;(2R)-2-[[(2R)-2-amino-3-(1-methoxycarbonylindol-3-yl)propanoyl]-[(2S)-2-[[(2R,6S)-2,6-dimethylpiperidine-1-carbonyl]amino]-4,4-dimethylpentanoyl]amino]hexanoate
Canonical SMILES CCCCC(C(=O)[O-])N(C(=O)C(CC1=CN(C2=CC=CC=C21)C(=O)OC)N)C(=O)C(CC(C)(C)C)NC(=O)N3C(CCCC3C)C.[Na+]
Formula C34H50N5NaO7 M.Wt 663.78
Solubility ≥ 33.2mg/mL in DMSO Storage Store at -20°C,protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.5065 mL 7.5326 mL 15.0652 mL
5 mM 0.3013 mL 1.5065 mL 3.013 mL
10 mM 0.1507 mL 0.7533 mL 1.5065 mL
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In vivo Formulation Calculator (Clear solution)

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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.
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.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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