(R)-BPO-27
Based on 3 publication(s) in Google Scholar
(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.
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- Pureté: 99.94%
- CAS No.: 1415390-47-4
- Formule: C26H18BrN3O6
- Masse moléculaire:548.34
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) (R)-BPO-27
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Activité biologique
IC50: 4 nM[1]
(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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female CD1 mice (age 8–10 wk)[3]
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Dosage:0.05, 0.15, 0.5, 1.5, and 5 mg/kg
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Administration:Intraperitoneal injection; 5 mg/kg; 30 min before abdominal surgery
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Result:Exhibited apparent efficacy in mice models of cholera and traveler’s diarrhea.
Chemical Information
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CAS No. 1415390-47-4
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Appearance Solid
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Masse moléculaire 548.34
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Formule C26H18BrN3O6
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Color White to off-white
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SMILES
O=C(C1=CC=C(O[C@@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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Gut Microbes
Increased intestinal permeability and downregulation of absorptive ion transporters Nhe3, Dra, and Sglt1 contribute to diarrhea during Clostridioides difficile infection. [Abstract]2023 Jan-Dec;15(1):2225841. PMID: 37350393 -
bioRxiv
Acute tuft cell ablation induces malabsorption and alterations in secretory and immune cell lineages in small intestine. [Abstract]2024 Sep 22:2024.09.18.613746. PMID: 39345424 -
bioRxiv
Altered cellular metabolic pathway and epithelial cell maturation induced by MYO5B defects are partially reversible by LPAR5 activation. [Abstract]2024 Sep 8:2024.09.03.610579. PMID: 39282272
Solvant et solubilité
DMSO : ≥ 14.28 mg/mL (26.04 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (287 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Snyder DS, et al. Absolute Configuration And Biological Properties of Enantiomers of CFTR Inhibitor BPO-27. ACS Med Chem Lett. 2013 May 9;4(5):456-459. [Content Brief]
[2]. Kim Y, et al. Benzopyrimido-pyrrolo-oxazine-dione (R)-BPO-27 Inhibits CFTR Chloride Channel Gating by Competition with ATP. Mol Pharmacol. 2015 Oct;88(4):689-96. [Content Brief]
[3]. Onur Cil, et al.Benzopyrimido-pyrrolo-oxazine-dione CFTR inhibitor (R)-BPO-27 for antisecretory therapy of diarrheas caused by bacterial enterotoxins. FASEB J. 2017 Feb;31(2):751-760. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8237 mL | 9.1184 mL | 18.2369 mL | 45.5921 mL |
| 5 mM | 0.3647 mL | 1.8237 mL | 3.6474 mL | 9.1184 mL | |
| 10 mM | 0.1824 mL | 0.9118 mL | 1.8237 mL | 4.5592 mL | |
| 15 mM | 0.1216 mL | 0.6079 mL | 1.2158 mL | 3.0395 mL | |
| 20 mM | 0.0912 mL | 0.4559 mL | 0.9118 mL | 2.2796 mL | |
| 25 mM | 0.0729 mL | 0.3647 mL | 0.7295 mL | 1.8237 mL |
(R)-BPO-27 Related Classifications
HY-19778 Related Classifications
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