1. Membrane Transporter/Ion Channel
    Autophagy
  2. CFTR
    Autophagy
  3. BPO-27 (racemate)

BPO-27 (racemate) 

Cat. No.: HY-19778A Purity: 98.37%
Handling Instructions

BPO-27 racemate is a potent CFTR inhibitor with an IC50 of 8 nM.

For research use only. We do not sell to patients.

BPO-27 (racemate) Chemical Structure

BPO-27 (racemate) Chemical Structure

CAS No. : 1314873-02-3

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10 mM * 1 mL in DMSO USD 507 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
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10 mg USD 600 In-stock
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100 mg USD 2520 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

BPO-27 racemate is a potent CFTR inhibitor with an IC50 of 8 nM.

IC50 & 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].

Molecular Weight

548.34

Formula

C₂₆H₁₈BrN₃O₆

CAS No.

1314873-02-3

SMILES

O=C(C1=CC=C(OC(C2=CC=C(Br)O2)C3=C(N(C)C4=O)C(C(N4C)=O)=C(C5=CC=CC=C5)N36)C6=C1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 6 mg/mL (10.94 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8237 mL 9.1184 mL 18.2369 mL
5 mM 0.3647 mL 1.8237 mL 3.6474 mL
10 mM 0.1824 mL 0.9118 mL 1.8237 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

BPO-27 (racemate)CFTRAutophagyCystic fibrosis transmembrane conductance regulatorInhibitorinhibitorinhibit

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