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BQ-788 sodium salt

ET B-receptor antagonist,potent and selective CAS# 156161-89-6

BQ-788 sodium salt

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Chemical structure

BQ-788 sodium salt

3D structure

Chemical Properties of BQ-788 sodium salt

Cas No. 156161-89-6 SDF Download SDF
PubChem ID 23693553 Appearance Powder
Formula C34H50N5NaO7 M.Wt 663.78
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 43 mg/mL (64.78 mM)
*"≥" means soluble, but saturation unknown.
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
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+]
Standard InChIKey JFIJJAJAXSAGIH-IVZJRGRDSA-M
Standard InChI InChI=1S/C34H51N5O7.Na/c1-8-9-16-28(31(42)43)39(29(40)25(35)18-23-20-37(33(45)46-7)27-17-11-10-15-24(23)27)30(41)26(19-34(4,5)6)36-32(44)38-21(2)13-12-14-22(38)3;/h10-11,15,17,20-22,25-26,28H,8-9,12-14,16,18-19,35H2,1-7H3,(H,36,44)(H,42,43);/q;+1/p-1/t21-,22+,25-,26+,28-;/m1./s1
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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of BQ-788 sodium salt

DescriptionPotent, selective ETB receptor antagonist (IC50 = 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells).

BQ-788 sodium salt Dilution Calculator

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BQ-788 sodium salt Molarity Calculator

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Preparing Stock Solutions of BQ-788 sodium salt

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.5065 mL 7.5326 mL 15.0652 mL 30.1305 mL 37.6631 mL
5 mM 0.3013 mL 1.5065 mL 3.013 mL 6.0261 mL 7.5326 mL
10 mM 0.1507 mL 0.7533 mL 1.5065 mL 3.013 mL 3.7663 mL
50 mM 0.0301 mL 0.1507 mL 0.3013 mL 0.6026 mL 0.7533 mL
100 mM 0.0151 mL 0.0753 mL 0.1507 mL 0.3013 mL 0.3766 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on BQ-788 sodium salt

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.

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References on BQ-788 sodium salt

International Union of Pharmacology. XXIX. Update on endothelin receptor nomenclature.[Pubmed:12037137]

Pharmacol Rev. 2002 Jun;54(2):219-26.

In mammals, the endothelin (ET) family comprises three endogenous isoforms, ET-1, ET-2, and ET-3. ET-1 is the principal isoform in the human cardiovascular system and remains the most potent and long-lasting constrictor of human vessels discovered. In humans, endothelins mediate their actions via only two receptor types that have been cloned and classified as the ET(A) and ET(B) receptors in the first NC-IUPHAR (International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification) report on nomenclature in 1994. This report was compiled before the discovery of the majority of endothelin receptor antagonists (particularly nonpeptides) currently used in the characterization of receptors and now updated in the present review. Endothelin receptors continue to be classified according to their rank order of potency for the three endogenous isoforms of endothelin. A selective ET(A) receptor agonist has not been discovered, but highly selective antagonists include peptides (BQ123, cyclo-[D-Asp-L-Pro-D-Val-L-Leu-D-Trp-]; FR139317, N- [(hexahydro-1-azepinyl)carbonyl]L-Leu(1-Me)D-Trp-3 (2-pyridyl)-D-Ala) and the generally more potent nonpeptides, such as PD156707, SB234551, L754142, A127722, and TBC11251. Sarafotoxin S6c, BQ3020 ([Ala(11,15)]Ac-ET-1((6-21))), and IRL1620 [Suc-(Glu(9), Ala(11,15))-ET-1((8-21))] are widely used synthetic ET(B) receptor agonists. A limited number of peptide (BQ788) and nonpeptide (A192621) ET(B) antagonists have also been developed. They are generally less potent than ET(A) antagonists and display lower selectivity (usually only 1 to 2 orders of magnitude) for the ET(B) receptor. Radioligands highly selective for either ET(A) ((125)I-PD151242, (125)I-PD164333, and (3)H-BQ123) or ET(B) receptors ((125)I-BQ3020 and (125)I-IRL1620) have further consolidated classification into only these two types, with no strong molecular or pharmacological evidence to support the existence of further receptors in mammals.

BQ-788, a selective endothelin ET(B) receptor antagonist.[Pubmed:12070534]

Cardiovasc Drug Rev. 2002 Winter;20(1):53-66.

We describe characteristics of a selective endothelin (ET) ET(B) receptor antagonist, BQ-788 [N-cis-2,6-dimethylpiperidinocarbonyl-L-gamma-methylleucyl-D-1-methoxycarbonyltry ptophanyl-D-norleucine], which is widely used to demonstrate the role of endogenous or exogenous ETs in vitro and in vivo. In vitro, BQ-788 potently and competitively inhibited (125)I-labeled ET-1 binding to ET(B) receptors in human Girrardi heart cells (hGH) with an IC(50) of 1.2 nM, but only poorly inhibited the binding to ET A receptors in human neuroblastoma cell line SK-N-MC cells (IC(50), 1300 nM). In isolated rabbit pulmonary arteries, BQ-788 showed no agonistic activity up to 10 microM and competitively inhibited the vasoconstriction induced by an ET(B)-selective agonist (pA(2), 8.4). BQ-788 also inhibited several bioactivities of ET-1, such as bronchoconstriction, cell proliferation, and clearance of perfused ET-1. Thus, it is confirmed that BQ-788 is a potent, selective ET(B) receptor antagonist. In vivo, in conscious rats, BQ-788, 3 mg/kg/h, i.v., completely inhibited a pharmacological dose of ET-1- or sarafotoxin6c (S6c) (0.5 nmol/kg, i.v.)-induced ET(B) receptor-mediated depressor, but not pressor responses. Furthermore, BQ-788 markedly increased the plasma concentration of ET-1, which is considered an index of potential ET(B) receptor blockade in vivo. In Dahl salt-sensitive hypertensive (DS) rats, BQ-788, 3 mg/kg/h, i.v., increased blood pressure by about 20 mm Hg. It is reported that BQ-788 also inhibited ET-1-induced bronchoconstriction, tumor growth and lipopolysaccharide-induced organ failure. These data suggest that BQ-788 is a good tool for demonstrating the role of ET-1 and ET(B) receptor subtypes in physiological and/or pathophysiological conditions.

Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788.[Pubmed:8197152]

Proc Natl Acad Sci U S A. 1994 May 24;91(11):4892-6.

We describe the characteristics of a potent and selective endothelin (ET) B-receptor antagonist, BQ-788 [N-cis-2,6-dimethylpiperidinocarbonyl-L-gamma-methylleucyl-D -1- methoxycarbonyltryptophanyl-D-norleucine]. In vitro, this compound potently and competitively inhibits 125I-labeled endothelin 1 (ET-1) binding to ETB receptors on human Girardi heart cells (IC50, 1.2 nM) but only poorly inhibits the binding to ETA receptors on human neuroblastoma cell line SK-N-MC cells (IC50, 1300 nM). In isolated rabbit pulmonary arteries, BQ-788 shows no agonist activity up to 10 microM and competitively antagonizes the vasoconstriction induced by an ETB-selective agonist, BQ-3020 (pA2, 8.4). In rat, an ETA-selective antagonist, BQ-123 (1 mg/kg, i.v.), does not affect transient depressor response to ET-1 (0.3 nmol/kg, i.v.) but potently inhibits following sustained pressor response; vice versa, BQ-788 (1 mg/kg, i.v.) abolishes the depressor response, resulting in a rapid onset of apparently enhanced pressor response. Thus, being a potent and selective ETB receptor antagonist, BQ-788 may be considered as a powerful tool for investigating the role of ET in physiological and pathological processes.

Description

BQ-788 (sodium salt) is a potent and selective ETB receptor antagonist, inhibiting ET-1 binding to ETB receptors with an IC50 of 1.2 nM in human Girrardi heart cells.

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