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BQ-788 sodium salt
ET B-receptor antagonist,potent and selective

Catalog No.B3278
Size Price Stock Qty
10mM (in 1mL DMSO)
$470.00
In stock
1mg
$150.00
In stock
5mg
$350.00
In stock
10mg
$500.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Chemical structure

BQ-788 sodium salt

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.

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Chemical Properties

Cas No. 156161-89-6 SDF Download SDF
Synonyms N/A
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 Desiccate at RT
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

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.