BQ-123

BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension[1][2][3].

Product Specifications

CAS Number

[136553-81-6]

UNSPSC

12352209

Hazard Statement

H302, H315, H319, H335

Target

Endothelin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/BQ-123.html

Purity

99.82

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(N[C@](C(N(CCC1)[C@]1([H])C2=O)=O)([H])CC(O)=O)[C@H](NC([C@@H](NC([C@H](N2)C(C)C)=O)CC(C)C)=O)CC3=CNC4=CC=CC=C34

Molecular Formula

C31H42N6O7

Molecular Weight

610.70

Precautions

H302, H315, H319, H335

References & Citations

[1]Ihara M, et al. In vitro biological profile of a highly potent novel endothelin (ET) antagonist BQ-123 selective for the ETA receptor. J Cardiovasc Pharmacol. 1992;20 Suppl 12:S11-S14.|[2]Sakamoto A, et al. Distinct subdomains of human endothelin receptors determine their selectivity to endothelinA-selective antagonist and endothelinB-selective agonists. J Biol Chem. 1993 Apr 25;268 (12) :8547-53.|[3]Erdogan H et al. The protective effects of endothelin-A receptor antagonist BQ-123 in pentylenetetrazole-induced seizure in rats. Hum Exp Toxicol, 2014 Oct, 33 (10) :1008-16.|[4]Zamora MA, et al. BQ123, an ETA receptor antagonist, inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells. Am J Respir Cell Mol Biol. 1993;9 (4) :429-433.|[5]Douglas SA, et al. BQ-123, a selective endothelin subtype A-receptor antagonist, lowers blood pressure in different rat models of hypertension. J Hypertens. 1994;12 (5) :561-567.