Name | GLPG1837 |
Synonyms | ABBV974 ABBV974 ABBV 974 GLPG1837 ABBV-974 GLPG 1837 ABBV 974 GLPG1837 ABBV-974 GLPG-1837 BMS-935177 GLPG 1837 1654725-02-6 GLPG-1837(ABBV-974) |
CAS | 1654725-02-6 |
Molecular Formula | C16H20N4O3S |
Molar Mass | 348.42 |
Density | 1.326±0.06 g/cm3(Predicted) |
Boling Point | 443.2±45.0 °C(Predicted) |
pKa | 11.21±0.10(Predicted) |
Storage Condition | -20℃ |
In vitro study | GLPG1837 has good in vitro ADME properties (ADME: aborption, distribution, metabolism, excretion), in the stability analysis of microsomes and hepatocytes, GLPG1837 has a lower Clint,unb, good cell permeability, no off-target inhibition of CYPs and hERG channels. |
In vivo study | The pharmacokinetic properties of GLPG1837 are good, with low Cl,unb and good oral bioavailability in rats and dogs. In rats and dogs, 1 mg/kg of GLPG1837 was injected intravenously with clearance rates (CL) of 1.92 and 0.32 L/h/kg, respectively. In rats T 1/2 is 1.84 hours, while in dogs T 1/2 is 3 hours. The oral bioavailability of GLPG1837 was 67% in rats and greater than 100 in dogs when administered by the oral route at 5 mg/kg. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.87 ml | 14.35 ml | 28.701 ml |
5 mM | 0.574 ml | 2.87 ml | 5.74 ml |
10 mM | 0.287 ml | 1.435 ml | 2.87 ml |
5 mM | 0.057 ml | 0.287 ml | 0.574 ml |
biological activity | GLPG1837 (ABBV-974) is a novel CFTR Potentiator with an EC50 of 3 nM for F508del. Compared to Ivacaftor, it has an enhancing effect on CFTR mutants with class III mutations. |
Target | Value |
CFTR(F508del) () | 3 nM(EC50) |
CFTR(G551D) () | 339 nM(EC50) |