CYP11B2-IN-1

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CYP11B2-IN-1 是一种 CYP11B2 抑制剂，IC50 为 2.3 nM。 CYP11B2-IN-1 抑制 CYP11B1，IC50 为 142 nM。

CYP11B2-IN-1 is a CYP11B2 inhibitor with IC50 of 2.3 nM. CYP11B2-IN-1 inhibits CYP11B1 with IC50 of 142 nM.(In Vitro):The IC50 of CYP11B2-IN-1 for CYP19 is 1021 nM.(In Vivo):CYP11B2-IN-1 dose-dependently produces aldosterone lowering efficacy without affecting cortisol levels in rhesus pharmacodynamic models. CYP11B2-IN-1 (0.01 and 0.3 mg/kg; i.v.) reduces aldosterone AUC of 62% and 95%, respectively.

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

In a rhesus pharmacodynamic model, CYP11B2-IN-1 (Compound 32) produces dose-dependent aldosterone lowering efficacy, with no apparent effect on cortisol levels. 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.

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Others

Other Targets

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1356479-78-1

311.36

C18H18FN3O

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (321.18 mM)

CC(C)(O)c1cncc(c1)-c1nc2ccc(F)cc2n1C1CC1

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(-20℃)

With Ice Pack

≥ 2 years