产品
编 号：F524347
分子式：C13H10FN3
分子量：227.24
分子式：C13H10FN3
分子量：227.24
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是否有货
10mM*1mL in DMSO
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1mg
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2mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 928134-65-0
产品详情
生物活性：
Osilodrostat (LCI699) is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat inhibits aldosterone and corticosterone synthesis. Osilodrostat has blood pressure lowering ability. Osilodrostat can be used for research of Cushing syndrome (CS).
体内研究：
Osilodrostat (LCI699；0.1-100 mg/kg；口服；一次) 抑制 Ang-II 和 ACTH 刺激的 Sprague Dawley 大鼠中的醛固酮和皮质酮合成。 Osilodrostat (LCI699；3-100 mg/kg；口服；每日一次，持续 52 周) 降低 dTG 大鼠的平均动脉压并延长生存期。Animal Model:Male Ang-II- and ACTH-stimulated Sprague Dawley rats
Dosage:0.1, 0.3, 1 and 3 mg/kg (Ang-II-stimulated rats) and 1, 3, 10, 30 and 100 mg/kg (ACTH-stimulated rats)
Administration:Oral administration; once
Result:Inhibited the increase in plasma aldosterone concentrations stimulated by Ang II or ACTH in a dose-dependent manner.
Animal Model:dTG rats
Dosage:3, 10, 30 and 100 mg/kg
Administration:Oral administration; daily, for 52 weeks
Result:Increased fractional LV (systolic and diastolic) shortening, normalized LV isovolumic relaxation time to RR (IVRT/RR) ratio and myocardial cell size and reduced LV weight in a dose-dependent manner.
体外研究：
Osilodrostat (LCI699；0.01-10 μM；HAC15 细胞、17 种原代人肾上腺皮质细胞培养物和垂体腺瘤细胞) 抑制皮质醇和醛固酮。Osilodrostat 可抑制皮质酮和 11-脱氧皮质醇的积累，并对肾上腺雄激素产生适度影响。
Osilodrostat (LCI699) is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat inhibits aldosterone and corticosterone synthesis. Osilodrostat has blood pressure lowering ability. Osilodrostat can be used for research of Cushing syndrome (CS).
体内研究：
Osilodrostat (LCI699；0.1-100 mg/kg；口服；一次) 抑制 Ang-II 和 ACTH 刺激的 Sprague Dawley 大鼠中的醛固酮和皮质酮合成。 Osilodrostat (LCI699；3-100 mg/kg；口服；每日一次，持续 52 周) 降低 dTG 大鼠的平均动脉压并延长生存期。Animal Model:Male Ang-II- and ACTH-stimulated Sprague Dawley rats
Dosage:0.1, 0.3, 1 and 3 mg/kg (Ang-II-stimulated rats) and 1, 3, 10, 30 and 100 mg/kg (ACTH-stimulated rats)
Administration:Oral administration; once
Result:Inhibited the increase in plasma aldosterone concentrations stimulated by Ang II or ACTH in a dose-dependent manner.
Animal Model:dTG rats
Dosage:3, 10, 30 and 100 mg/kg
Administration:Oral administration; daily, for 52 weeks
Result:Increased fractional LV (systolic and diastolic) shortening, normalized LV isovolumic relaxation time to RR (IVRT/RR) ratio and myocardial cell size and reduced LV weight in a dose-dependent manner.
体外研究：
Osilodrostat (LCI699；0.01-10 μM；HAC15 细胞、17 种原代人肾上腺皮质细胞培养物和垂体腺瘤细胞) 抑制皮质醇和醛固酮。Osilodrostat 可抑制皮质酮和 11-脱氧皮质醇的积累，并对肾上腺雄激素产生适度影响。
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