Osilodrostat phosphate LCI699 phosphate|cas:1315449-72-9|西域试剂

Osilodrostat phosphate LCI699 phosphate,99.35%

产品编号：Bellancom-16276A| CAS NO：1315449-72-9| 分子式：C₁₃H₁₃FN₃O₄P| 分子量：325.23

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-16276A	￥1100.00	杭州北京（现货）
Bellancom-16276A	￥1600.00	杭州北京（现货）
Bellancom-16276A	￥2700.00	杭州北京（现货）
Bellancom-16276A	￥4900.00	杭州北京（现货）
Bellancom-16276A	￥8500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

Osilodrostat phosphate LCI699 phosphate

产品介绍

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。

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).

体外研究

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.

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

体内研究

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.
Osilodrostat (LCI699; 3-100 mg/kg; p.o.; daily, for 52 weeks) phosphate reduces mean arterial pressure and prolongs survival in dTG rats.

西域 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
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.

体内研究

西域 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
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.

性状

Solid

溶解性数据

In Vitro:

H₂O : ≥ 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
10 mM	0.3075 mL	1.5374 mL	3.0747 mL

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。

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)

参考文献