BQ 788 sodium salt

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Description: Selective ETB antagonist
Chemical Name: N-[(cis-2,6-Dimethyl-1-piperidinyl)carbonyl]-4-methyl-L-leucyl-1-(methoxycarbonyl)-D-tryptophyl-D-norleucine sodium salt
Purity: ≥95% (HPLC)
Datasheet
Citations (8)
Reviews
Literature (4)

Biological Activity for BQ 788 sodium salt

BQ 788 sodium salt is a potent, selective ETB receptor antagonist (IC50 = 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells).

Technical Data for BQ 788 sodium salt

M. Wt 663.79
Formula C34H50N5NaO7
Storage Desiccate at -20°C
Purity ≥95% (HPLC)
CAS Number 156161-89-6
PubChem ID 16759603
InChI Key QCVIFBRTTLMEOV-FUKQNADPSA-M
Smiles [Na+].CCCC[C@@H](NC(=O)[C@@H](CC1=CN(C(=O)OC)C2=C1C=CC=C2)NC(=O)[C@H](CC(C)(C)C)NC(=O)N1[C@@H](C)CCC[C@H]1C)C([O-])=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for BQ 788 sodium salt

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 3.32 5
DMSO 3.32 5

Preparing Stock Solutions for BQ 788 sodium salt

The following data is based on the product molecular weight 663.79. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.05 mM 30.13 mL 150.65 mL 301.3 mL
0.25 mM 6.03 mL 30.13 mL 60.26 mL
0.5 mM 3.01 mL 15.07 mL 30.13 mL
2.5 mM 0.6 mL 3.01 mL 6.03 mL

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Product Datasheets for BQ 788 sodium salt

Certificate of Analysis / Product Datasheet
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References for BQ 788 sodium salt

References are publications that support the biological activity of the product.

Davenport (2002) International Union of Pharmacology. XXIX. Update on endothelin receptor nomenclature. Pharmacol.Rev. 54 219 PMID: 12037137

Ishikawa et al (1994) Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788. Proc.Natl.Acad.Sci.U.S.A. 91 4892 PMID: 8197152

Okada and Nishikibe (2002) BQ-788, a selective endothelin ETB receptor antagonist. Cardiovasc.Drug Rev. 20 53 PMID: 12070534


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Keywords: BQ 788 sodium salt, BQ 788 sodium salt supplier, Selective, ETB, antagonists, Receptors, Endothelin, BQ788, sodium, salt, 1500, Tocris Bioscience

8 Citations for BQ 788 sodium salt

Citations are publications that use Tocris products. Selected citations for BQ 788 sodium salt include:

Yeligar et al (2009) Ethanol-induced expression of ET-1 and ET-BR in liver sinusoidal endothelial cells and human endothelial cells involves hypoxia-inducible factor-1alpha and microrNA-199. J Immunol 183 5232 PMID: 19783678

Sánchez et al (2014) Endothelin-1 contributes to endothelial dysfunction and enhanced vasoconstriction through augmented superoxide production in penile arteries from Ins-resistant obese rats: role of ET(A) and ET(B) receptors. Br J Pharmacol 171 5682 PMID: 25091502

Ou et al (2014) Adaptive regulation of endothelin receptor type-A and type-B in vascular smooth muscle cells during pregnancy in rats. J Cell Physiol 229 489 PMID: 24105843

Allahdadi et al (2010) Endothelin-1 induces contraction of female rat internal pudendal and clitoral arteries through ET(A) receptor and rho-kinase activation. PLoS One 7 2096 PMID: 20412427


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Literature in this Area

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