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BPO-27 racemate (BPO-27 (racemate)) is an effective CFTR inhibitor with IC50 of 8 nM.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $39 | In Stock | |
5 mg | $119 | In Stock | |
10 mg | $178 | In Stock | |
25 mg | $295 | In Stock | |
50 mg | $431 | In Stock | |
100 mg | $595 | In Stock | |
200 mg | $798 | In Stock | |
1 mL x 10 mM (in DMSO) | $137 | In Stock |
Description | BPO-27 racemate (BPO-27 (racemate)) is an effective CFTR inhibitor with IC50 of 8 nM. |
Targets&IC50 | CFTR:8 nM |
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 [1]. (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 [2]. |
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 [1]. |
Alias | BPO-27 (racemate) |
Molecular Weight | 548.34 |
Formula | C26H18BrN3O6 |
Cas No. | 1314873-02-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 55 mg/mL (100.3 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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