BPO-27 racemate
Modify Date: 2024-01-21 15:17:48
BPO-27 racemate structure
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Common Name | BPO-27 racemate | ||
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| CAS Number | 1314873-02-3 | Molecular Weight | 548.34 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C26H18BrN3O6 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of BPO-27 racemateBPO-27 racemate is a potent CFTR inhibitor with an IC50 of 8 nM. |
| Name | BPO-27 racemate |
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| Synonym | More Synonyms |
| Description | BPO-27 racemate is a potent CFTR inhibitor with an IC50 of 8 nM. |
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| Related Catalog | |
| Target |
IC50: 8 nM[1] |
| In Vitro | The benzopyrimido-pyrrolo-oxazinedione BPO-27 is an analogue of PPQ-102, which inhibits CFTR with an IC50 of 8 nM. The R enantiomer of BPO-27 inhibits CFTR chloride conductance with an IC50 of 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 shows 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 interperitoneal administration in mice, serum (R)-1 decays with t1/2 ≈ 1.6 h and gives sustained therapeutic concentrations in kidney[1]. |
| Cell Assay | Whole-cell recordings are done on CFTR-expressing CHO-K1 cells. After establishing the whole-cell configuration, BPO-27 is added for 5 minutes, and then CFTR is activated by the addition of forskolin (10 μM) in the continued presence of BPO-27 (0.5 or 1 μM). Whole-cell currents are elicited by applying hyperpolarizing and depolarizing voltage pulses from a holding potential of 0 mV to potentials between +80 and −80 mV in steps of 20 mV. Recordings are made at room temperature using an Axopatch-200B. Currents are digitized with a Digidata 1440A converter and filtered at 5 kHz[2]. |
| Animal Admin | Mice: (R)-BPO-27 is formulated at 1 mg/mL in 5% DMSO, 2.5% Tween-80 and 2.5% PEG400 in water. Male mice in a CD1 genetic background are administered 300 μL of the (R)-BPO-27 formulation by intraperitoneal injection. At specified times, blood samples are collected by eye bleed. At 4 h, kidneys are removed following renal arterial perfusion with PBS. Kidneys are weighed, mixed with acetic acid and homogenized for analysis[1]. |
| References |
| Molecular Formula | C26H18BrN3O6 |
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| Molecular Weight | 548.34 |
| Storage condition | 2-8℃ |
| BPO-27 (racemate) |