[CAS NO. 1654725-02-6] GLPG1837
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PRODUCTS SPECIFICATIONS [1654725-02-6]
Store
Catalog
SLK-S8698
Brand
Selleck
CAS
1654725-02-6
DESCRIPTION [1654725-02-6]
Overview
| MDL | MFCD31630754 |
|---|---|
| Molecular Weight | 348.42 |
| Molecular Formula | C16H20N4O3S |
| SMILES | O=C(C1=NNC=C1)NC(S2)=C(C(N)=O)C3=C2C(C)(C)OC(C)(C)C3 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8701 mL | 14.3505 mL | 28.7010 mL |
| 5 mM | 0.5740 mL | 2.8701 mL | 5.7402 mL |
| 10 mM | 0.2870 mL | 1.4350 mL | 2.8701 mL |
| 50 mM | 0.0574 mL | 0.2870 mL | 0.5740 mL |
Description
GLPG1837 (ABBV-974) is a novel potentiator with an EC50 value of 3 nM for F508del, showing enhanced efficacy on CFTR mutants harboring class III mutations compared to Ivacaftor.
In vitro
GLPG1837 has an attractive in vitro ADME profile, showing low Clint,unb in both microsomal and hepatocytes stability assays, good permeability, and no off-target inhibition of CYPs and the hERG channel.
In vivo
The pharmacokinetic profile of GLPG1837 is attractive, showing a low Cl,unb and good F% in both rat and dog. The CL (L/h/kg) of GLPG1837 after intravenous injection of 1 mg/kg dose are 1.92 and 0.32 in rats and dogs, respectively. T is 1.84 h in rats while 3 h in dogs. After 5 mg/kg p.o, the oral availability of GLPG1837 in rat is 67%. In dogs, F%>100.
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