PG01
Based on 1 Customer Validation
PG01 is a potent CFTR Cl- channel potentiator. PG01 can correct gating defects of CFTR mutants, is effective on b>E193K, G970R and G551D (CFTR mutants) with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively. PG01 is also effective on ΔF508 (Ka of 0.3 μM). PG01 increases ΔF508-CFTR Cl- current after adding Forskolin.
For research use only. We do not sell to patients.
- Purity: 98.04%
- CAS No.: 853138-65-5
- Formula: C28H29N3O2
- Molecular Weight:439.55
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
CFTR[1]
PG01 itself does not activate F508-CFTR, produces substantial F508-CFTR Cl- current after the addition of 0.5 and 2 μM Forskolin. PG01 at 100 nM strongly stimulates channel activity with multiple channel openings observed. The apparent Kd for PG01 for G551D-CFTR activation is 1 μM, approximately 100-fold better than that of genistein. The potency for activation G1349D-CFTR by PG01 is even better at 40 nM. PG01 produces large currents in both G551D- and G1349D-CFTR expressing cells. The currents are sensitive to CFTRinh-172 and are not seen in nontransfected cells[1].
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.
Chemical Information
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CAS No. 853138-65-5
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Appearance Solid
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Molecular Weight 439.55
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Formula C28H29N3O2
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Color White to off-white
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SMILES
O=C(N(C)C(C1=CC=CC=C1)C(NC2=CC=C(C(C)C)C=C2)=O)CC3=CNC4=C3C=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 43.96 mg/mL (100.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (273 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Pedemonte N, et al. Phenylglycine and sulfonamide correctors of defective delta F508 and G551D cystic fibrosis transmembrane conductance regulator chloride-channel gating. Mol Pharmacol. 2005 May;67(5):1797-807. [Content Brief]
[2]. Caputo A, et al. Mutation-specific potency and efficacy of cystic fibrosis transmembrane conductance regulator chloride channel potentiators. J Pharmacol Exp Ther. 2009 Sep;330(3):783-91. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2751 mL | 11.3753 mL | 22.7505 mL | 56.8764 mL |
| 5 mM | 0.4550 mL | 2.2751 mL | 4.5501 mL | 11.3753 mL | |
| 10 mM | 0.2275 mL | 1.1375 mL | 2.2751 mL | 5.6876 mL | |
| 15 mM | 0.1517 mL | 0.7584 mL | 1.5167 mL | 3.7918 mL | |
| 20 mM | 0.1138 mL | 0.5688 mL | 1.1375 mL | 2.8438 mL | |
| 25 mM | 0.0910 mL | 0.4550 mL | 0.9100 mL | 2.2751 mL | |
| 30 mM | 0.0758 mL | 0.3792 mL | 0.7584 mL | 1.8959 mL | |
| 40 mM | 0.0569 mL | 0.2844 mL | 0.5688 mL | 1.4219 mL | |
| 50 mM | 0.0455 mL | 0.2275 mL | 0.4550 mL | 1.1375 mL | |
| 60 mM | 0.0379 mL | 0.1896 mL | 0.3792 mL | 0.9479 mL | |
| 80 mM | 0.0284 mL | 0.1422 mL | 0.2844 mL | 0.7110 mL | |
| 100 mM | 0.0228 mL | 0.1138 mL | 0.2275 mL | 0.5688 mL |
PG01 Related Classifications
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