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|---|---|---|
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| Cat. No. : | HY-122744 |
| M.Wt: | 266.30 |
| Formula: | C16H14N2O2 |
| Purity: | >98 % |
| Solubility: |
CYP11B1-IN-1 is a selective, orally active hCYP11B1 inhibitor, with an IC50 of 2 nM against hCYP11B1 and an IC50 of 1.8 μM against rat CYP11B1. CYP11B1-IN-1 can be used for the research of Cushing's disease[1].
In Vitro:CYP11B1-IN-1 (Compound 25) potently inhibits hCYP11B1 (IC50 = 2 nM), and exhibits 14-fold higher selectivity for hCYP11B1 over hCYP11B2 in V79MZ hamster fibroblasts expressing recombinant enzymes[1].
CYP11B1-IN-1 inhibits rat CYP11B1, with an IC50 of 1.8 μM in V79MZ hamster fibroblasts expressing this recombinant enzyme[1].
CYP11B1-IN-1 (1 μM; 0-60 min) exhibits superior metabolic stability in rat liver S9 fractions, with a half-life of 23 min, which is better than that of Ref 7 and metyrapone[1].
CYP11B1-IN-1 (6.25-100 μM; 66 h) shows no cytotoxicity in HEK293 cells, with an IC20 value of up to 42 μM[1].
CYP11B1-IN-1 (up to 100 μM) shows no mutagenic potential in *Salmonella typhimurium* strains TA98 and TAMix, with or without metabolic activation by rat liver S9 fraction[1].
CYP11B1-IN-1 (3.16 μM; 48 h) does not activate the aryl hydrocarbon receptor in HepG2 cells[1].
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