BPO-27 racemate

SKU: orb1309909

Description

BPO-27 racemate

Research Area

Cell Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1314873-02-3
• MW: 548.34
• Purity: 98.19%
• Formula: C₂₆H₁₈BrN₃O₆
• SMILES: Cn1c2c3C(Oc4ccc(cc4-n3c(-c3ccccc3)c2c(=O)n(C)c1=O)C(O)=O)c1ccc(Br)o1
• Target: Autophagy,CFTR
• Solubility: 10% DMSO+90% Corn Oil:1.67 mg/mL (3.05 mM);DMSO:55 mg/mL (100.3 mM)

Bioactivity

• Target IC50:
  CFTR:8 nM
• In Vivo:
  Following bolus intraperitoneal administration of BPO-27 in mice, serum (R)-1 decays with t1/2 ≈ 1.6 h and gives sustained therapeutic concentrations in the kidney .
• In Vitro:
  The R enantiomer of BPO-27 inhibits CFTR chloride conductance (IC50: 4 nM), while S enantiomer is inactive. In vitro metabolic stability in hepatic microsomes shows both enantiomers as stable, with less than 5% metabolism in 4 h . (R)-BPO-27 binds near the canonical ATP binding site. Whole-cell patch-clamp studies show linear CFTR currents with a voltage-independent (R)-BPO-27 block mechanism. At a concentration of (R)-BPO-27 that inhibits CFTR chloride current by 50%, the EC50 for ATP activation of CFTR increases from 0.27 to 1.77 mM .

Storage & Handling

• Storage: 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

racemate, inhibit, Inhibitor, Autophagy, BPO 27, BPO 27 racemate, BPO27, BPO-27, BPO-27 (racemate), BPO27 racemate, BPO-27 racemate, Cystic fibrosis transmembrane conductance regulator, CFTR

Compound Identifiers

PubChem CID

53387352