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Osilodrostat (Synonyms: LCI699) 纯度: 99.90%
Osilodrostat (LCI699) 是人11β-羟化酶和醛固酮合成酶的有效抑制剂,IC50分别值为2.5 和0.7nM。
Osilodrostat Chemical Structure
CAS No. : 928134-65-0
规格 | 价格 | 是否有货 | 数量 |
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥875 | In-stock | |
2 mg | ¥700 | In-stock | |
5 mg | ¥1000 | In-stock | |
10 mg | ¥1500 | In-stock | |
25 mg | ¥2500 | In-stock | |
50 mg | ¥4900 | In-stock | |
100 mg | ¥8500 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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生物活性 |
Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase and aldosterone synthase with IC50 values of 2.5 and 0.7 nM, respectively. |
IC50 & Target |
IC50: 2.5 nM (human 11β-hydroxylase), 0.7 nM (aldosterone synthase)[1] |
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体内研究 (In Vivo) |
Osilodrostat and pasireotide monotherapies are associated with significant changes in the histology and mean weights of the pituitary and adrenal glands, liver, and ovary/oviduct. Osilodrostat alone is associated with adrenocortical hypertrophy and hepatocellular hypertrophy. In combination, osilodrostat/pasireotide does not exacerbate any target organ changes and ameliorated the liver and adrenal gland changes observed with monotherapy. Cmax and AUC0–24h of osilodrostat and pasireotide increase in an approximately dose-proportional manner[1]. Osilodrostat treatment reduces urinary free cortisol in patients with Cushing’s disease; 78.9% has normal urinary free cortisol at week 22. Treatment with osilodrostat is generally well tolerated[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
227.24 |
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Formula |
C13H10FN3 |
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CAS 号 |
928134-65-0 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 250 mg/mL (1100.16 mM; Need ultrasonic) Ethanol : 100 mg/mL (440.06 mM; Need ultrasonic) 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Animal Administration [1] |
Rats: Sixty male and 60 female rats are randomized into single-sex groups to receive daily doses of pasireotide (0.3 mg/kg/day, subcutaneously), osilodrostat (20 mg/kg/day, orally), osilodrostat/pasireotide in combination (low dose, 1.5/0.03 mg/kg/day; mid-dose, 5/0.1 mg/kg/day; or high dose, 20/0.3 mg/kg/day), or vehicle for 13 weeks[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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参考文献 |
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