BQ-123

SKU: orb1226438

Description

BQ-123 (PMZ 2123) is a potent, selective, non-competitive cyclic pentapeptide ETA receptor antagonist with IC50 of 7.3 nM; antagonizes endothelin-1-induced contractions in rabbit aorta, increases in inositol phosphates in cultured rat vascular smooth muscle A10 cells, shifts concentration-response curves in isolated rabbit aorta elicited by angiotensin II, but does not bind to angiotensin II receptors nor affect angiotensin II-induced increases in inositol phosphates.Diabetes Phase 1 Clinical(In Vivo):Sustained infusions of BQ-123 (0.16-164 nmol/kg per min, intravenously, for 6 h) produces dose-dependent reductions in mean arterial pressure in spontaneously hypertensive rats (SHR), the maximal reduction being obtained with a dose of 16 nmol/kg per min.BQ-123 (3 mg/kg; i.v.; given 15 minutes before pentylenetetrazole (PTZ)) impedes the formation and spread of seizure to a great degree in PTZ (50 mg/kg; i.p.) +BQ-123 groups.

Key Properties

• CAS Number: 136553-81-6
• MW: 610.7012
• Purity: >98% (HPLC)
• Formula: C₃₁H₄₂N₆O₇
• SMILES: O=C(O)C[C@H]1NC([C@@H](CC2=CNC3=C2C=CC=C3)NC([C@H](CC(C)C)NC([C@@H](C(C)C)NC([C@@](CCC4)([H])N4C1=O)=O)=O)=O)=O
• Target: Endothelin Receptor
• Solubility: DMSO: ≥ 34 mg/mL

Bioactivity

• In Vivo:
  Animal model: Male Wistar albino rats. Dosage: 3 mg/kg. Administration: Intravenous injection; given 15 minutes before PTZ. Result: Number of rats with major seizure decreased.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PMZ 2123 | BQ123

Quick Database Links

Gene Symbol

Endothelin Receptor