Information 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. Targets CFTR(F508del) ; CFTR(G551D) 3 nM(EC50); 339 nM(EC50) 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 1/2 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.
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GLPG1837
Dangerous GoodsCAS number：1654725-02-6 molecular formula：C16H20N4O3S
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | D80376 | ABBV-974; GLPG-1837 | ABBV974 | ABBV 974 | 1654725-02-6 | BDBM50246760 | GLPG 1837 | N-(3-carbamoyl-5,5,7,7-tetramethyl-4,7-dihydro-5H-thieno[2,3-c]pyran-2-yl)-1H-pyrazole-3-carboxamide | HY-111099 | N-(3-carbamoyl-5,5,7,7-tetramethyl-4H-thieno[2 | ||
| CAS number | 1654725-02-6 | molecular formula | C16H20N4O3S |
| molecular weight | 348.42 g/mol | Exact mass | ≥98% |
| PSA | 138.000 Ų | logp | 1.800 |
numbering system
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physicochemical properties
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激
Statement of Preventive Measures：
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。
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MSDS
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