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(R)-BPO-27

Name: (R)-BPO-27
Brand: TargetMol
SKU: T10591L
Rating: 4.5 (1 reviews)

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Catalog No. T10591LCas No. 1415390-47-4

(R)-BPO-27 is an orally active and potent ATP-competitive CFTR inhibitor (IC50: 4 nM) for the study of diarrhoea and polycystic kidney.

(R)-BPO-27

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Purity: 99.1%

Catalog No. T10591LCas No. 1415390-47-4

(R)-BPO-27 is an orally active and potent ATP-competitive CFTR inhibitor (IC50: 4 nM) for the study of diarrhoea and polycystic kidney.

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
1 mg	$147	5 days	5 days

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Purity:99.1%

Appearance:Solid

Color:White

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COA LCMS

Product Introduction

Bioactivity

Description	(R)-BPO-27 is an orally active and potent ATP-competitive CFTR inhibitor (IC50: 4 nM) for the study of diarrhoea and polycystic kidney.
Targets&IC50	forskolin-stimulated CFTR Cl-current:4 nM (in FRT cells)
In vitro	In HEK-293T cells, (R)-BPO-27 exhibits a dose-response inhibition and inhibits the CFTR current by 50% at 0.53 nM. Acting from the cytoplasmic side, (R)-BPO-27 has low membrane permeability[3].In a single-channel patch-clamp experiment with HEK-293T cells expressing human wild-type CFTR, (R)-BPO-27 reduces the channel open probability (NPo) from 0.29 to 0.08. It modestly reduces the mean channel open time and strongly increases the mean channel closed time. In contrast, (S)-BPO-27 does not affect any of these parameters[3].(R)-BPO-27 is directly applied to the cytoplasmic membrane surface and stabilizes the CFTR channel closed state with an IC50 of 600 pM in a single-channel electrophysiology assay[2].In CFTR-expressing FRT cells after CFTR stimulation by cAMP agonist, (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. It also shows an IC50 of 4 nM for inhibition of forskolin-stimulated CFTR Cl- current in FRT cells[1].
In vivo	In a PK study, (R)-BPO-27 (intraperitoneal administration; 10 mg/kg) decays with a t1/2≈1.6 h and provides sustained therapeutic concentrations in the kidney[3]. Preventing fluid accumulation in closed midjejunal loops produced by cholera toxin, (R)-BPO-27 (intraperitoneal injection; 5 mg/kg; 30 min before abdominal surgery) yields an intestinal loop weight/length ratio similar to that in PBS-injected loops. This effect is dose-dependent, with an IC50 value of 0.1 mg/kg[1]. Administered via intraperitoneal injection or oral administration at 5 mg/kg, (R)-BPO-27 demonstrates slow metabolism and maintains sustained serum levels for at least 4 hours. Oral bioavailability of (R)-BPO-27 in mouse pharmacokinetics and toxicity study is approximately 94% based on AUC analysis[1].

Chemical Properties

Molecular Weight	548.34
Formula	C₂₆H₁₈BrN₃O₆
Cas No.	1415390-47-4
Smiles	Cn1c2c3[C@@H](Oc4ccc(cc4-n3c(-c3ccccc3)c2c(=O)n(C)c1=O)C(O)=O)c1ccc(Br)o1
Relative Density.	1.68 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 10 mg/mL (18.24 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8237 mL	9.1184 mL	18.2369 mL	91.1843 mL
5 mM	0.3647 mL	1.8237 mL	3.6474 mL	18.2369 mL
10 mM	0.1824 mL	0.9118 mL	1.8237 mL	9.1184 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc