1. Metabolic Enzyme/Protease
    Autophagy
  2. FXR
    Autophagy
  3. Tropifexor

Tropifexor (Synonyms: LJN452)

製品番号: HY-107418 純度: 99.35%
取扱説明書

Tropifexor (LJN452) is a highly potent agonist of FXR with an EC50 of 0.2 nM.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用としては使用しないように、十分ご注意ください。

Tropifexor 構造式

Tropifexor 構造式

CAS 番号 : 1383816-29-2

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 252 在庫あり
Estimated Time of Arrival: December 31
1 mg USD 100 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 190 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 290 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 790 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 1250 在庫あり
Estimated Time of Arrival: December 31
200 mg USD 1850 在庫あり
Estimated Time of Arrival: December 31
500 mg   お問い合わせ  
1 g   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 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

Tropifexor (LJN452) is a highly potent agonist of FXR with an EC50 of 0.2 nM[1].

IC50 & Target

EC50: 0.2 nM (FXR)

体外実験

Tropifexor (compound 1) is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM. Robust induction of both BSEP and SHP genes is observed in primary cells by Tropifexor in a concentration-dependent manner.
BSEP induction above vehicle (DMSO) control is observed at concentrations as low as 1 nM, while strong induction of SHP (15-fold above vehicle) is observed at 10 nM and modest induction of SHP at 1 nM (3-fold)[1].

体内実験

Tropifexor (compound 1) demonstrates highly potent induction of SHP and FGF15 in the ileum as doses as low as 0.1 mg/kg. In the liver, robust induction of SHP is observed at 0.01 mg/kg of Tropifexor with maximal levels of gene induction achieved at 0.3 mg/kg. Expression of CYP8B1 mRNA following 14 day treatment with Tropifexor is already apparent at the lowest dose (0.003 mg/kg), and CYP8B1 gene expression is fully repressed at doses above 0.03 mg/kg.
Treatment of rats with Tropifexor exhibits a clear dose-dependent increase in plasma FGF15 protein, with maximal levels of FGF15 detected at 7 h postdose.
Treatment with Tropifexor for 14 days produces a robust dose-dependent reduction in serum triglycerides and reaches a maximal response with a 0.3 mg/kg dose, resulting in a decrease of triglyceride levels to approximately 79% below the vehicle control group[1].

臨床実験
分子量

603.58

分子式

C₂₉H₂₅F₄N₃O₅S

CAS 番号

1383816-29-2

SMILES

FC(F)(F)OC(C=CC=C1)=C1C2=NOC(C3CC3)=C2CO[[email protected]@H]4C[[email protected]]5N(C6=NC7=C(F)C=C(C(O)=O)C=C7S6)[[email protected]](CC5)C4

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 : ≥ 80.66 mg/mL (133.64 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6568 mL 8.2839 mL 16.5678 mL
5 mM 0.3314 mL 1.6568 mL 3.3136 mL
10 mM 0.1657 mL 0.8284 mL 1.6568 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 (4.14 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.14 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
細胞実験
[1]

Primary rat hepatocytes are plated in 24 well plates and incubated with a 5 point dose response of Tropifexor (compound 1) for 24 hours. RNA is harvested from the cells using the RNeasy 96 kit. Quantitative PCR is performed. The fold change of the transcript over no stimulation is calculated using the ΔΔCt method, with DMSO (vehicle control) being no stimulation[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。

動物実験
[1]

Adult male wild-type Sprague-Dawley rats are used in this study. All animals are fasted for 3 hours before oral dosing with Tropifexor (compound 1) or with vehicle. Tropifexor is administered orally using a range of four doses (0.03, 0.1, 0.3, and 1.0 mg/kg) and compare directly to the vehicle control group (vehicle: 0.5% methylcellulose, 0.5% Tween 80, 99% water, suspension). Animals are sacrificed seven hours after dosing using CO2, liver, ileum and whole blood (in heparinized tubes) samples are collected for analysis[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

純度: 99.35%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • モル濃度カルキュレーター

  • 希釈カルキュレーター

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

TropifexorLJN452LJN 452LJN-452FXRAutophagyNR1H4Inhibitorinhibitorinhibit

最近チェックした製品:

オンラインお問い合わせ

Your information is safe with us. * Required Fields.

製品名

 

タイトル

お名前 *

 

PC 用メールアドレス *

電話番号 *

 

勤務先/学校名 *

Department *

 

カスタマ需要量 *

国会或いは地域 *

     

必ず会社名を記載ください。個人への返信は行いません。

メッセージ

バルクお問い合わせ

Inquiry Information

製品名:
Tropifexor
製品番号:
HY-107418
数量:
MCE 日本正規代理店: