bq-788

Description: BQ788 is a novel, potent and selectiveETB (endothelin B) receptor antagonist, attenuating stab woundinjury-induced reactive astrocytes in rat brain and inhibiting ET-1binding to ETB receptors with an IC50 of 1.2 nM in human Girrardi heartcells. BQ788 were well tolerated and showed signs of directly andindirectly reducing the viability of melanoma cells.

References:

1. Okada M, et al. BQ-788, a selective endothelin ET(B) receptor antagonist. Cardiovasc Drug Rev. 2002 Winter; 20(1):53-66.

2. SargentCA, et al. Effect of endothelin antagonists with or without BQ 788 onET-1 responses in pithed rats. J Cardiovasc Pharmacol. 1995; 26 Suppl3:S216-8.

3. FattoriV, et al. Differential regulation of oxidative stress and cytokineproduction by endothelin ETA and ETB receptors in superoxideanion-induced inflammation and pain in mice. J Drug Target. 2016 Oct5:1-27

4. First-in-Human Proof-of-Concept Study: IntralesionalAdministration of BQ788, an Endothelin Receptor B Antagonist, to Melanoma SkinMetastases. Oncologist. 2015 Oct; 20(10):1121-2. doi:10.1634/theoncologist.2015-0139. Epub 2015 Sep 1. PubMed PMID: 26330458; PubMedCentral PMCID: PMC4591941.