SR-1903
SR-1903 is an inverse agonist of RORγ and PPARγ (IC50 of ∼100 nM and 209 nM for RORγ and PPARγ, respectively) and a LXR agonist. SR-1903 exhibits anti-inflammatory and anti-diabetic efficacy in collagen-induced arthritis and diet-induced obesity mouse models.
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- No. CAS: 1414248-06-8
- Fòrmula: C27H27F6N3O
- Peso molecular:523.51
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
RORγ ~100 nM (IC50) |
PPARγ 209 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
70 nM
Compound: 16
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Displacement of [3H]T0901317 from human RoRc expressed in HepG2 cells by scintillation proximity binding assay
Displacement of [3H]T0901317 from human RoRc expressed in HepG2 cells by scintillation proximity binding assay
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[PMID: 24502334] |
In Vitro
SR1903 (10 μM) attenuates LPS (HY-D1056) signaling in macrophages, with suppression of TREM-1 gene expression[1].
SR1903 increases expression of LXR target genes, including genes involved in macrophage cholesterol efflux (ABCG1 and SCD) and lipid metabolism (ACACA and FASN) in macrophage RAW264.7[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SR1903 (20 mg/kg, i.p., 14 days) improves metabolic parameters and protects against obesity-associated thymic degeneration in diet-induced obese (DIO) mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Collagen-induced arthritis (female DBA/1J mice were injected with chicken type II collagen on day 1, and then each animal received a boost injection of collagen on day 21)[1]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection (i.p.), twice-a-day for a total of 16 days
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Result:Demonstrated a reduction in arthritis clinic score at the conclusion of the study (day 34).
Did not cause enlargement of the liver.
Had enhanced thymocyte differentiation and survival compared to mice treated with either the selective LXR agonist GW3965 or the dual LXR agonist/RORγ inverse agonist T0901317.
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Animal Model:Diet-induced obese (DIO) mouse (Male, 22 weeks of age, fed a high fat diet (60% kCal % fat))[1]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection (i.p.), 14 days
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Result:Improved fasting glucose levels and reduced total cholesterol and low density lipoprotein (LDL).
Improved both fasting and fed insulin levels.
Showed 15% weight loss and 17% reduction in fat mass after 14 days.
Reduced food intake.
Reduced leptin resistance and repressed Socs3 (suppressor of cytokine signaling-3) expression.
Chemical Information
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No. CAS 1414248-06-8
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Peso molecular 523.51
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Fòrmula C27H27F6N3O
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SMILES
OC(C(F)(F)F)(C(F)(F)F)C1=CC=C(C2=CC=C(CN3CCN(CC4=CC=NC=C4)CC3)C=C2C)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SR-1903 Related Classifications
HY-138007 Related Classifications
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