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1356479-78-1

1356479-78-1 structure
1356479-78-1 structure
  • Name: CYP11B2-IN-1
  • Chemical Name: CYP11B2-IN-1
  • CAS Number: 1356479-78-1
  • Molecular Formula: C18H18FN3O
  • Molecular Weight: 311.35
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Cytochrome P450
  • Create Date: 2020-04-07 19:09:42
  • Modify Date: 2024-01-10 06:45:38
  • 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].

Name CYP11B2-IN-1
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
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.

Molecular Formula C18H18FN3O
Molecular Weight 311.35
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