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

(R)-BPO-27 

Cat. No.: HY-19778 Purity: 99.86%
Handling Instructions

(R)-BPO-27, the R enantiomer of BPO-27, is a potent, orally active and ATP-competitive CFTR inhibitor with an IC50 of 4 nM.

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

(R)-BPO-27 Chemical Structure

(R)-BPO-27 Chemical Structure

CAS No. : 1415390-47-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 507 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

(R)-BPO-27, the R enantiomer of BPO-27, is a potent, orally active and ATP-competitive CFTR inhibitor with an IC50 of 4 nM.

IC50 & Target

IC50: 4 nM[1]

In Vitro

(R)-BPO-27 exhibits a dose-response inhibition and inhibits the CFTR current by 50% at 0.53 nM in HEK-293T cells. (R)-BPO-27 acts from the cytoplasmic side and has low membrane permeability[1].
(R)-BPO-27 reduces the channel open probability (NPo) from 0.29 to 0.08, modestly reduces in mean channel open time, and strongly increases mean channel closed time in HEK-293T cells expressing human wild-type CFT in a single-channel patch-clamp experiment. Meanwhile, (S)-BPO-27 does not affect any of these parameters[1].
(R)-BPO-27 is applied directly to the cytoplasmic membrane surface and stabilizes the CFTR channel closed state with an IC50 of 600 pM in Single-channel electrophysiology assay[2].
(R)-BPO-27 (10 μM, 10 min pretreatment) inhibits Cl- current with apparent IC50 values of 5 and 10 nM for CPT-cAMP and 8-Br-cGMP, respectively, in CFTR-expressing FRT cells after CFTR stimulation by cAMP agonist. the IC50 of 4 nM for inhibition of forskolin-stimulated CFTR Cl- current in FRT cells[3].

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

In Vivo

(R)-BPO-27 (interperitoneal administration; 10 mg/kg) decays with t1/2≈1.6 h and gives sustained therapeutic concentrations in kidney in a PK study[1].
(R)-BPO-27 (intraperitoneal injection; 5 mg/kg; 30 min before abdominal surgery) prevents fluid accumulation in closed midjejunal loops produced by cholera toxin, giving an intestinal loop weight/length ratio similar to that in PBS-injected loops. This effect is dose-dependently and the IC50 value is 0.1 mg/kg[3].
(R)-BPO-27 (intraperitoneal injection or oral administration; 5 mg/kg) shows a slow (R)-BPO-27 metabolism and produces sustained serum (R)-BPO-27 levels for at least 4 h. The AUC analysis gave an oral bioavailability of ∼94% for (R)-BPO-27 in mouse pharmacokinetics and toxicity study[3].

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

Animal Model: Female CD1 mice (age 8–10 wk)[3]
Dosage: 0.05, 0.15, 0.5, 1.5, and 5 mg/kg
Administration: Intraperitoneal injection; 5 mg/kg; 30 min before abdominal surgery
Result: Exhibited apparent efficacy in mice models of cholera and traveler’s diarrhea.
Molecular Weight

548.34

Formula

C₂₆H₁₈BrN₃O₆

CAS No.

1415390-47-4

SMILES

O=C(C1=CC=C(O[[email protected]@H](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 : ≥ 14.28 mg/mL (26.04 mM)

*"≥" means soluble, but saturation unknown.

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
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Keywords:

(R)-BPO-27CFTRAutophagyCystic fibrosis transmembrane conductance regulatorR enantiomerbacterialenterotoxinantisecretoryCHO-K1fluid accumulationcholeratraveler’s diarrheaInhibitorinhibitorinhibit

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