BQ-788

BQ-788 is a potent, selective ETB receptor antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC cells with IC50 of 1300 nM[1].

Product Specifications

CAS Number

[173326-37-9]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Endothelin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Cardiovascular Disease; Endocrinology; Cancer

Assay Protocol

https://www.medchemexpress.com/BQ-788.html

Purity

99.70

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CCCC[C@H](C(O)=O)NC([C@@H](CC1=CN(C(OC)=O)C2=CC=CC=C12)NC([C@H](CC(C)(C)C)NC(N3[C@H](C)CCC[C@@H]3C)=O)=O)=O

Molecular Formula

C34H51N5O7

Molecular Weight

641.80

Precautions

H302, H315, H319, H335

References & Citations

[1]Okada M, et al. BQ-788, a selective endothelin ET (B) receptor antagonist. Cardiovasc Drug Rev. 2002 Winter;20 (1) :53-66.|[2]Sargent CA, et al. Effect of endothelin antagonists with or without BQ 788 on ET-1 responses in pithed rats. J Cardiovasc Pharmacol. 1995;26 Suppl 3:S216-8.|[3]Fattori V, et al. Differential regulation of oxidative stress and cytokine production by endothelin ETA and ETB receptors in superoxide anion-induced inflammation and pain in mice. J Drug Target. 2016 Oct 5:1-27

Shipping Conditions

Blue Ice

Storage Conditions

-20°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Phase 1

Isoform

ETB

Citation 01

Cells. 2021 Nov 8;10 (11) :3072.|Environ Pollut. 2016 Feb:209:11-20.|Environ Pollut. 2016 Nov:218:487-496.|J Exp Clin Cancer Res. 2025 Feb 21;44 (1) :64.|Neurotherapeutics. 2021 Oct;18 (4) :2664-2681.|Toxicol Sci. 2016 Jan;149 (1) :213-26.|BMC Cancer. 2018 Feb 6;18 (1) :154.|Environ Sci Pollut Res Int. 2018 May;25 (15) :14713-14725.|J Neuroimmune Pharmacol. 2024 Apr 13;19 (1) :13.|PLoS Pathog. 2020 Oct 19;16 (10) :e1008947.