BQ 788 sodium salt

Catalog # Availability Size / Price Qty
1500/1
BQ 788 sodium salt | CAS No. 156161-89-6 | Endothelin ETB Receptor Antagonists
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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%

Product Details
Citations (8)
Supplemental Products
Reviews (1)

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

M.Wt:
663.79
Formula:
C34H50N5NaO7
Solubility:
Soluble to 5 mM in DMSO
Purity:
≥95%
Storage:
Store 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. 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):.
  2. International Union of Pharmacology. XXIX. Update on endothelin receptor nomenclature.
    Davenport
    Pharmacol.Rev., 2002;54:219
  3. 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
  4. 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

  1. 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
  2. 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
  3. Activation of the endothelin system mediates pathological angiogenesis during ischemic retinopathy.
    Authors: Patel Et al.
    J Sex Med  2014;184:3040
  4. 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
  5. 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
  6. 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
  7. 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
  8. 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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Product works great
By Anonymous on 11/02/2017

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!


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