RS-2982
Based on 1 Customer Validation
RS-2982 is a retinoic acid receptor-related orphan receptor A (RORA) agonist. RS-2982 enhances the promoter activity of MIR122 via the RORA binding site, and promotes the expression and secretion of MIR122. RS-2982 reduces the expression of hepatic triglyceride biosynthetic enzymes, hepatic lipotoxicity, hepatic fibrosis and body weight in diet-fed mice, while improving insulin resistance. RS-2982 can be used in the research of non-alcoholic steatohepatitis.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 98.88%
- CAS 番号: 440120-55-8
- 分子式: C26H25N3O2
- 分子量:411.50
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
RORA |
体外実験
RS-2982 (1 μM; 24 h) promotes secretion of MIR122 from Huh7 cells without altering intracellular MIR122 levels or causing cytotoxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:human hepatocellular carcinoma Huh7 cells
-
Concentration:1 μM
-
Incubation Time:24 h
-
Result:Did not change cellular MIR122 levels.
Significantly increased secretion of MIR122 into the culture medium.
Caused no significant cytotoxicity via LDH release.
Parmacokinetics
| Species | Dose | Route | T1/2 |
|---|---|---|---|
| Mice[1] | 7.5 mg/kg | i.p. | 2.7 h |
体内実験
RS-2982 (7.5 mg/kg; i.p.; single dose) increases hepatic and systemic MIR122 levels and modulates MIR122 target gene expression in healthy mice for up to 7 days post-administration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6 (male, 7-8 weeks old, fed 50% high-fat diet for 4 weeks to induce NAFLD)[1]
-
Dosage:7.5 mg/kg
-
Administration:i.p.; twice weekly; 3 weeks
-
Result:Restored hepatic RORA mRNA levels to those seen in normal diet-fed mice.
Significantly reduced mouse body weight, liver weight, hepatic lipid droplets, and hepatic triglyceride (TG) content.
Increased plasma β-hydroxybutyrate levels.
Significantly increased hepatic pri-MIR122 and pre-MIR122 levels, while reduced hepatic MIR122 target genes (Agpat1, Dgat1); increased hepatic RORA target gene Fgf21.
Increased mature MIR122 levels in plasma and skeletal muscle, reduced MIR122 target genes (AldoA, Agpat1) and muscle TG content in skeletal muscle.
Reversed the antagomiR-122-induced body weight gain and restored body weight to control levels when co-administered with antagomiR-122.
-
Animal Model:C57BL/6 (male, 7-8 weeks old, fed 50% high-fat diet for 6 weeks to induce established NAFLD)[1]
-
Dosage:15 mg/kg
-
Administration:i.p.; three times weekly; 3 weeks
-
Result:Significantly increased mature MIR122 levels in liver and plasma, as well as hepatic pri-MIR122, pre-MIR122, and RORA target genes (Fgf21, G6PC).
Reduced mouse body weight, liver-to-body weight ratio, hepatic lipid droplets, and hepatic TG content.
Improved insulin tolerance.
Increased total energy expenditure and fat oxidation in metabolic cages.
Reduced white adipose tissue inflammation, as shown by decreased mRNA levels of F4/80, IFNβ, and TNFα.
-
Animal Model:C57BL/6 (male, 7-8 weeks old, fed atherogenic diet for 3 weeks to induce NASH with fibrosis)[1]
-
Dosage:15 mg/kg
-
Administration:i.p.; three times weekly; 3.5 weeks
-
Result:Significantly reduced plasma AST and ALT levels, and increased mature MIR122 levels in liver and plasma.
Reduced liver inflammation (decreased CD3+ and F4/80+ cell staining) and liver fibrosis (decreased Masson Trichrome and α-SMA staining), alongside a reduction in hepatic NK1.1+ cells.
Significantly reduced hepatic mRNA levels of fibrosis driver genes (Acta1, Col1A1, Col3A1, TgfbR2, Tgfb2), while increased RORA target gene Fgf21.
-
Animal Model:C57BL/6 (male, 7-8 weeks old, normal diet-fed)[1]
-
Dosage:7.5 mg/kg
-
Administration:i.p.; single dose
-
Result:Significantly increased mature MIR122 levels in liver (days 1, 7), plasma (days 1, 2, 7), white adipose tissue (days 1, 2), skeletal muscle (days 1, 2), and heart (day 2).
Increased hepatic pri-MIR122 and pre-MIR122 levels, while reduced hepatic MIR122 target gene AldoA and increased RORA target gene G6PC.
Significantly reduced cardiac MIR122 target genes (Agpat1, AldoA, Dgat1).
化学情報
-
CAS 番号 440120-55-8
-
性状 Solid
-
分子量 411.50
-
分子式 C26H25N3O2
-
Color Light yellow to yellow
-
SMILES
O=C1NC2=CC(C(N3CCC(CC3)CC4=CC=CC=C4)=O)=CC=C2NC5=C1C=CC=C5
-
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
純度とドキュメンテーション
-
データシート (280 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
RS-2982 関連分類
HY-187422 関連分類
Powered by Bioz