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

Osilodrostat (Synonyms: LCI699)

製品番号: HY-16276 純度: 99.04%
取扱説明書

Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase and aldosterone synthase with IC50 values of 2.5 and 0.7 nM, respectively.

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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
10 mM * 1 mL in DMSO USD 87 在庫あり
Estimated Time of Arrival: December 31
2 mg USD 70 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 100 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 150 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 250 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 490 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 850 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

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Based on 1 publication(s) in Google Scholar

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製品説明

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]

体内実験

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].

臨床実験
分子量

227.24

分子式

C₁₃H₁₀FN₃

CAS 番号

928134-65-0

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: 

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

DMSO : ≥ 83.3 mg/mL (366.57 mM)

*"≥" means soluble, but saturation unknown.

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 provided by MCE.
参考文献
動物実験
[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].

MCE はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献
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Keywords:

OsilodrostatLCI699LCI 699LCI-699Mineralocorticoid ReceptorInhibitorinhibitorinhibit

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Inquiry Information

製品名:
Osilodrostat
製品番号:
HY-16276
数量:
MCE 日本正規代理店: