BQ-123

SKU: orb1300461

Description

BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM. This compound is a valuable research tool for investigating the role of ET-1 signaling in cardiovascular diseases, pulmonary hypertension, and cancer, as demonstrated in various in vitro and in vivo studies. It has been evaluated in Phase 2 clinical trials.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 136553-81-6
• MW: 610.7
• Purity: 99.22% (May vary between batches)
• Formula: C₃₁H₄₂N₆O₇
• SMILES: [H][C@@]12CCCN1C(=O)[C@@]([H])(CC(O)=O)NC(=O)[C@@H](Cc1c[nH]c3ccccc13)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](NC2=O)C(C)C
• Target: Endothelin Receptor
• Solubility: Ethanol:12 mg/mL (19.65 mM);DMSO:93 mg/mL (152.28 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (8.19 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  ETA receptor:7.3 nM
• In Vivo:
  In rats, BQ-123 (1 mg/kg, i.v.) ameliorates myocardial ischemic-reperfusion injury. In rats with pentylenetetrazole (PTZ)-induced tonic-clonic seizures, BQ-123 (3 mg/kg, i.v.) potently impedes the formation and spread of seizure. In pregnant C57BL/6 mice, BQ-123 (6.7 mg/kg, i.p.) prevents LPS-induced preterm birth in mice via the induction of uterine and placental IL-10.
• In Vitro:
  In porcine aortic vascular smooth muscle cells, BQ-123 selectively inhibits ETA-mediated contraction. In rat vascular smooth muscle cells, BQ-123 inhibits endothelin-1-induced phosphoinositide breakdown and DNA synthesis.

Storage & Handling

• Storage: keep away from moisture,keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cells, BQ 123, BQ123, BQ-123, blood, artery, EndothelinReceptor, Endothelin Receptor, Endothelin A receptor, Inhibitor, inhibit, muscle, smooth, pulmonary, pressure

Compound Identifiers

PubChem CID

443289