CYP11B2-IN-1 |
Katalog-Nr.GC70725 |
CYP11B2-IN-1 ist ein CYP11B2-Inhibitor mit einem IC50 von 2,3 nM.
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Cas No.: 1356479-78-1
Sample solution is provided at 25 µL, 10mM.
CYP11B2-IN-1 (Compound 32) also inhibits CYP19 with an IC50 of 1021 nM [1] .
In a rhesus pharmacodynamic model, CYP11B2-IN-1 (Compound 32) produces dose-dependent aldosterone lowering efficacy, with no apparent effect on cortisol levels[1].
CYP11B2-IN-1also displays a good rhesus pharmacokinetics profile, with low plasma clearance and acceptable oral exposure.When dosed i.v. at 0.01 and 0.3 mg/kg, CYP11B2-IN-1 produces reductions in aldosterone AUC of 62% and 95%, respectively, compared to baseline[1].
References:
[1]. Hoyt SB, et al. Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.ACS Med Chem Lett. 2015 Apr 7;6(5):573-8.
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