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GLPG2451 is an enhancer of cystic fibrosis transmembrane conductance regulator (CFTR) and effectively enhances cryo-rescued F508del CFTR with an EC50 of 11.1 nM.
| Molecular Weight | 419.38 |
| Formula | C16H16F3N3O5S |
| CAS Number | 2055015-61-5 |
| Solubility (25°C) | DMSO ≥ 200 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related CFTR Products |
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| CP-628006
The CFTR potentiator CP-628006 enhances CFTR function in cystic fibrosis patient-derived air chamber cells by a mechanism of action different from that of existing potentiators such as ivacaftor. |
| Icenticaftor
Icenticaftor (QBW251) is an oral enhancer of the cystic fibrosis transmembrane conductance regulator (CFTR) channel with an EC50 of 79 nM for F508del and 497 nM for G551D CFTR. Icenticaftor can be used in chronic obstructive pulmonary disease (COPD) and cystic fibrosis studies. |
| NJH-2-057
NJH-2-057 is a conjugate of the deubiquitinase OTUB1 covalent ligand-linked lumacaftor, which stabilizes mutant CFTR proteins in cells. |
| FDL169
FDL169 is a CFTR corrector that is designed to fix and restore the function of the defective CFTR protein. |
| Nesolicaftor
Nesolicaftor (PTI-428) is a specific cystic fibrosis transmembrane conductance regulator (CFTR) amplifier. |
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