BQ 788 sodium salt
Chemical Name: N-[(cis-2,6-Dimethyl-1-piperidinyl)carbonyl]-4-methyl-L-leucyl-1-(methoxycarbonyl)-D-tryptophyl-D-norleucine sodium salt
Purity: ≥95%
Biological Activity
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
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.
Background References
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The endothelin B receptor plays a crucial role for the adhesion of neutrophils to the endothelium in sickle cell disease
B Koehl, P Nivoit, W El Nemer, O Lenoir, P Hermand, C Pereira, V Brousse, L Guyonnet, G Ghinatti, M Benkerrou, Y Colin, C Le Van Kim, PL Tharaux
Haematologica, 2017;0(0):. -
International Union of Pharmacology. XXIX. Update on endothelin receptor nomenclature.
Davenport
Pharmacol.Rev., 2002;54:219 -
Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788.
Ishikawa et al.
Proc.Natl.Acad.Sci.U.S.A., 1994;91:4892 -
BQ-788, a selective endothelin ETB receptor antagonist.
Okada and Nishikibe
Cardiovasc.Drug Rev., 2002;20:53
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Citations for BQ 788 sodium salt
The citations listed below are publications that use Tocris products. Selected citations for BQ 788 sodium salt include:
8 Citations: Showing 1 - 8
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Increased cerebrovascular sensitivity to endothelin-1 in a rat model of obstructive sleep apnea: a role for endothelin receptor B.
Authors: Durgan Et al.
J Cereb Blood Flow Metab 2015;35:402
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Adaptive regulation of endothelin receptor type-A and type-B in vascular smooth muscle cells during pregnancy in rats.
Authors: Ou Et al.
J Cell Physiol 2014;229:489
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Activation of the endothelin system mediates pathological angiogenesis during ischemic retinopathy.
Authors: Patel Et al.
J Sex Med 2014;184:3040
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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.
Authors: Sánchez Et al.
Br J Pharmacol 2014;171:5682
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Endothelin-1 induces contraction of female rat internal pudendal and clitoral arteries through ET(A) receptor and rho-kinase activation.
Authors: Allahdadi Et al.
PLoS One 2010;7:2096
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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.
Authors: Yeligar Et al.
J Immunol 2009;183:5232
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Transcriptional regulation of monocyte chemotactic protein-1 release by endothelin-1 in human airway smooth muscle cells involves NF-kappaB and AP-1.
Authors: Sutcliffe Et al.
Br J Pharmacol 2009;157:436
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Endothelin-1 activates ETA receptors to cause reflex scratching in BALB/c mice.
Authors: McQueen Et al.
Br J Pharmacol 2007;151:278
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We utilized this product at 1uM to inhibit endothelin-B receptors ex vivo in mouse aortas followed by vasomotor function experiments. We have obtained superior results using this BQ788 product!
