BQ 788 sodium salt

Cat. No. 1500

BQ 788 sodium salt C34H50N5NaO7 [156161-89-6]

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Chemical Name: N-[(cis-2,6-Dimethyl-1-piperidinyl)carbonyl]-4-methyl-L-leucyl-1-(methoxycarbonyl)-D-tryptophyl-D-norleucine sodium salt

Biological Activity

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

Technical Data

M.Wt:
663.79
Formula:
C34H50N5NaO7
Solubility:
Soluble to 5 mM in ethanol and to 5 mM in DMSO
Purity:
>95 %
Storage:
Desiccate at -20°C
CAS No:
156161-89-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

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

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

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.

If you know of a relevant reference for this product please let us know.

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

Durgan et al (2015) Increased cerebrovascular sensitivity to endothelin-1 in a rat model of obstructive sleep apnea: a role for endothelin receptor B. J Cereb Blood Flow Metab 35 402. PMID: 25425077.

Patel et al (2014) Activation of the endothelin system mediates pathological angiogenesis during ischemic retinopathy. J Sex Med 184 3040. PMID: 25203536.

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.

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.

McQueen et al (2007) Endothelin-1 activates ETA receptors to cause reflex scratching in BALB/c mice. Br J Pharmacol 151 278. PMID: 17351652.

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

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