1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  2. Mineralocorticoid Receptor
  3. Osilodrostat phosphate

Osilodrostat phosphate  (Synonyms: LCI699 phosphate)

目录号: HY-16276A 纯度: 99.35%
COA 产品使用指南

Osilodrostat (LCI699) phosphate 是一种口服有效的 11β-羟化酶 (CYP11B1) 抑制剂,其 IC50 值为 35 nM。Osilodrostat phosphate 是一种口服有效的醛固酮合成酶 (CYP11B2) 抑制剂,抑制人醛固酮合成酶和大鼠醛固酮合成酶的 IC50 分别为 0.7 nM 和 160 nM。Osilodrostat phosphate 抑制醛固酮和皮质酮的合成。Osilodrostat phosphate 具有降低血压的能力。Osilodrostat phosphate 可用于库欣综合征 (CS) 的研究。

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Osilodrostat phosphate Chemical Structure

Osilodrostat phosphate Chemical Structure

CAS No. : 1315449-72-9

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Osilodrostat (LCI699) phosphate is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat phosphate 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 phosphate inhibits aldosterone and corticosterone synthesis. Osilodrostat phosphate has blood pressure lowering ability. Osilodrostat phosphate can be used for research of Cushing syndrome (CS)[1][2][3].

IC50 & Target

IC50: 35 nM (CYP11B1), 0.7 nM (human aldosterone synthase), and 160 nM (rat aldosterone synthase)[1][2]

体外研究
(In Vitro)

Osilodrostat (LCI699; 0.01-10 µM; HAC15 cells, 17 primary human adrenocortical cell cultures, and pituitary adenoma cells) phosphate inhibits cortisol and aldosterone. Osilodrostat results in inhibition of corticosterone, 11-deoxycortisol accumulation, and modest effects on adrenal androgens[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Osilodrostat (LCI699; 0.1-100 mg/kg; p.o.; once) phosphate inhibits aldosterone and corticosterone synthesis in Ang-II- and ACTH-stimulated Sprague Dawley rats[1].
Osilodrostat (LCI699; 3-100 mg/kg; p.o.; daily, for 52 weeks) phosphate reduces mean arterial pressure and prolongs survival in dTG rats[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Ang-II- and ACTH-stimulated Sprague Dawley rats[1]
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[1]
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.
Clinical Trial
分子量

325.23

Formula

C13H13FN3O4P

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O 中的溶解度 : ≥ 200 mg/mL (614.95 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0747 mL 15.3737 mL 30.7475 mL
5 mM 0.6149 mL 3.0747 mL 6.1495 mL
查看完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献

完整储备液配制表

* 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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 3.0747 mL 15.3737 mL 30.7475 mL 76.8687 mL
5 mM 0.6149 mL 3.0747 mL 6.1495 mL 15.3737 mL
10 mM 0.3075 mL 1.5374 mL 3.0747 mL 7.6869 mL
15 mM 0.2050 mL 1.0249 mL 2.0498 mL 5.1246 mL
20 mM 0.1537 mL 0.7687 mL 1.5374 mL 3.8434 mL
25 mM 0.1230 mL 0.6149 mL 1.2299 mL 3.0747 mL
30 mM 0.1025 mL 0.5125 mL 1.0249 mL 2.5623 mL
40 mM 0.0769 mL 0.3843 mL 0.7687 mL 1.9217 mL
50 mM 0.0615 mL 0.3075 mL 0.6149 mL 1.5374 mL
60 mM 0.0512 mL 0.2562 mL 0.5125 mL 1.2811 mL
80 mM 0.0384 mL 0.1922 mL 0.3843 mL 0.9609 mL
100 mM 0.0307 mL 0.1537 mL 0.3075 mL 0.7687 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Osilodrostat phosphate
目录号:
HY-16276A
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