GLPG1837 GLPG1837 (ABBV-974) is a novel CFTR potentiator with an EC50 value of 3 nM for F508del, showing enhanced efficacy on CFTR mutants harboring class III mutations compared to Ivacaftor.TargetsCFTR(F508del) ; CFTR(G551D) 3 nM(EC50); 339 nM(EC50)In vitroGLPG1837 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 vivoThe 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. T1/2 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.
Specification: ≥98%
Molecular Formula: C16H20N4O3S
Molecular Weight: 348.42
PubChem CID: 117857370
Isomeric SMILES: CC1(CC2=C(C(O1)(C)C)SC(=C2C(=O)N)NC(=O)C3=CC=NN3)C
Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/G414121-SCI_7619d866861a79838dadb92bde0f3eea.pdf
- UPC:
- 12352202
- Condition:
- New
- Availability:
- 1 day
- Weight:
- 0.06 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- G414121-2mg
- CAS:
- 1654725-02-6
- Product Size:
- 2mg
- Hazard Statement Codes:
- H335:H319:H315
- Precautionary Statement Codes:
- P305+P351+P338:P261
