RS-2982
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.
For research use only. We do not sell to patients.
- CAS No.: 440120-55-8
- Formula: C26H25N3O2
- Molecular Weight:411.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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RORA |
RS-2982 (0.5-5 μM; 48 h) potently and specifically activates wild-type MIR122 promoter activity in Huh7 cells via RORA, with significant induction observed at concentrations of 0.5 μM, 1 μM, and 5 μM[1].
RS-2982 (1 μM; 24 h) promotes secretion of MIR122 from Huh7 cells without altering intracellular MIR122 levels or causing cytotoxicity[1].
RS-2982 has moderate cytotoxicity in Huh7 and CEM cells, with CC50 values of 10.4 μM and 11.0 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human hepatocellular carcinoma Huh7 cells
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Concentration:1 μM
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Incubation Time:24 h
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Result:Did not change cellular MIR122 levels.
Significantly increased secretion of MIR122 into the culture medium.
Caused no significant cytotoxicity via LDH release.
| Species | Dose | Route | T1/2 |
|---|---|---|---|
| Mice[1] | 7.5 mg/kg | i.p. | 2.7 h |
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].
RS-2982 (15 mg/kg; i.p.; three times weekly; 3 weeks) reverses established NAFLD in HFD-fed mice by increasing MIR122 expression, reducing body weight and hepatic steatosis, improving insulin sensitivity, and enhancing energy expenditure and fat oxidation[1].
RS-2982 (15 mg/kg; i.p.; three times weekly; 3.5 weeks) reduces liver inflammation and fibrosis in atherogenic diet-fed mice via upregulation of MIR122, while improving liver enzyme levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 7-8 weeks old, fed 50% high-fat diet for 4 weeks to induce NAFLD)[1]
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Dosage:7.5 mg/kg
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Administration:i.p.; twice weekly; 3 weeks
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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.
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Animal Model:C57BL/6 (male, 7-8 weeks old, fed 50% high-fat diet for 6 weeks to induce established NAFLD)[1]
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Dosage:15 mg/kg
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Administration:i.p.; three times weekly; 3 weeks
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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.
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Animal Model:C57BL/6 (male, 7-8 weeks old, fed atherogenic diet for 3 weeks to induce NASH with fibrosis)[1]
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Dosage:15 mg/kg
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Administration:i.p.; three times weekly; 3.5 weeks
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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.
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Animal Model:C57BL/6 (male, 7-8 weeks old, normal diet-fed)[1]
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Dosage:7.5 mg/kg
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Administration:i.p.; single dose
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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).
Chemical Information
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CAS No. 440120-55-8
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Molecular Weight 411.50
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Formula C26H25N3O2
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SMILES
O=C1NC2=CC(C(N3CCC(CC3)CC4=CC=CC=C4)=O)=CC=C2NC5=C1C=CC=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RS-2982 Related Classifications
HY-187422 Related Classifications
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