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PG 01 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator. Corrects gating defects of CFTR mutants such as ΔF508 (Ka = 0.3 μM), E193K and G970R (Kd values are 0.22 μM and 0.45 μM respectively). Increases ΔF508-CFTR Cl- currents in the presence of forskolin; displays no effect on Ca2+-activated Cl- current.
| Molecular Weight | 439.55 |
| Formula | C28H29N3O2 |
| CAS Number | 853138-65-5 |
| Solubility (25°C) | DMSO 43.95 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CFTR Products |
|---|
| Ataluren
Ataluren (PTC124) is a novel, orally available small molecular CFTR-G542X nonsense allele inhibitor. |
| VX-770 (Ivacaftor)
VX-770 (Ivacaftor) is a first-in-class potentiator of CFTR, which targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM, respectively. |
| Lonidamine
Lonidamine (AF-1890) is a novel CFTR open channel blocker with an IC50 of 0.85 mM, which inhibits aerobic glycolysis in cancer cells. Lonidamine (AF-1890) is a hexokinase and mitochondrial pyruvate carrier inhibitor (Ki=2.5 μM). |
| VX-809
VX-809 is a CFTR corrector that improves CFTR processing and maturation in the cell. |
| CFTR(inh)-172
CFTR(inh)-172 is a voltage-independent, selective CFTR inhibitor with Ki of 300 nM, showing no effects on MDR1, ATP-sensitive K+ channels, or a series of other transporters. |
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