1. Metabolic Enzyme/Protease
  2. Mineralocorticoid Receptor
  3. Osilodrostat

Osilodrostat  (Synonyms: LCI699)

製品番号: HY-16276 純度: 99.90%
COA 取扱説明書

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).

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Osilodrostat 構造式

Osilodrostat 構造式

CAS 番号 : 928134-65-0

容量 価格(税別) 在庫状況 数量
Solution
10 mM * 1 mL in DMSO USD 96 在庫あり
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 96 在庫あり
Estimated Time of Arrival: December 31
Solid
2 mg USD 77 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 110 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 165 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 275 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 539 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 935 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 2 publication(s) in Google Scholar

Other Forms of Osilodrostat:

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製品説明

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)[1][2][3].

IC50 & Target

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

体外実験

Osilodrostat (LCI699; 0.01-10 µM; HAC15 cells, 17 primary human adrenocortical cell cultures, and pituitary adenoma cells) 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.

体内実験

Osilodrostat (LCI699; 0.1-100 mg/kg; p.o.; once) 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) 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.
臨床実験
分子量

227.24

分子式

C13H10FN3

CAS 番号
SMILES

N#CC1=CC=C([[email protected]]2CCC3=CN=CN32)C(F)=C1

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 250 mg/mL (1100.16 mM; Need ultrasonic)

Ethanol : 100 mg/mL (440.06 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.4006 mL 22.0032 mL 44.0063 mL
5 mM 0.8801 mL 4.4006 mL 8.8013 mL
10 mM 0.4401 mL 2.2003 mL 4.4006 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (11.00 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (11.00 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (11.00 mM); Clear solution

  • 4.

    Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (11.00 mM); Clear solution

  • 5.

    Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (11.00 mM); Clear solution

  • 6.

    Add each solvent one by one:  10% EtOH    90% corn oil

    Solubility: ≥ 2.5 mg/mL (11.00 mM); Clear solution

*All of the co-solvents are available by MCE.
純度とドキュメンテーション

純度: 99.90%

参考文献
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製品名:
Osilodrostat
製品番号:
HY-16276
数量:
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