CYP11B2-IN-1

Names

[ CAS No. ]:
1356479-78-1

[ Name ]:
CYP11B2-IN-1

Biological Activity

[Description]:

CYP11B2-IN-1 is a CYP11B2 inhibitor with an IC50 of 2.3 nM. CYP11B2-IN-1 inhibits CYP11B1 with an IC50 of 142 nM[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> Cytochrome P450

[Target]

CYP11B2:2.3 nM (IC50)

CYP11B1:142 nM (IC50)

[In Vitro]

CYP11B2-IN-1 (Compound 32) also inhibits CYP19 with an IC50 of 1021 nM [1] 。

[In Vivo]

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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₈H₁₈FN₃O

[ Molecular Weight ]:
311.35

Related Compounds

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