Gala-SR
Gala-SR (Gala-SR1078) is an RORα agonist. Gala-SR ameliorates rhythm disorders by enhancing the amplitude of the circadian rhythm. Gala-SR can be used for the study of periodontitis.
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- No. CAS: 3092129-97-7
- Fòrmula: C24H22F9NO8
- Peso molecular:623.42
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Chemical Information
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Actividad biológica
Descripciòn
IC50 & Target
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RORα |
In Vitro
Gala-SR (1-100 μM, 24-72 h) significantly improved Human U2OS cell compatibility through galactose modification[1].
Gala-SR (5 μM, 24 h) significantly upregulates the mRNA expression of G6Pase and FGF21, direct target genes of RORα/γ, in HepG2 cells[1].
Gala-SR (5 μM) selectively enhances RORα transcriptional activation activity in HEK293T cells[1].
Gala-SR (5 μM, 24 h) shows significantly reduced activation effects on the G6Pase and FGF21 genes after RORα is knocked down[1].
Gala-SR (5 μM) targets and activates RORα primarily through its hydrolyzable galactose modification[1].
Gala-SR (2-5 μM) significantly enhances the bioluminescence levels and rhythmic amplitude of the BMAL1 and Per2 reporter genes in U2OS cells, and enhances the expression of the BMAL1 protein[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Upregulated the mRNA expression of G6Pase and FGF21, direct target genes of RORα/γ, in HepG2 cells.
Parmacokinetics
In Vivo
Gala-SR (10 mg/kg, lights on, once) enhances liver luciferase signaling in PER2::LUC knock-in mice, indicating enhanced BMAL1 expression[1].
Gala-SR (10 mg/kg, i.p., once daily for 3 weeks) restores the amplitude of periodontal tissue rhythm in periodontal mice with periodontitis, inhibits the NF-κB inflammatory pathway, and alleviates periodontitis-related bone loss[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice were first acclimatized to a 12-hour light/12-hour dark (L:D) condition for 2 weeks, and then switched to continuous darkness (D:D) to induce circadian rhythm disorder[1].
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Dosage:10 mg/kg
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Administration:1 hour before the end of the light exposure, i.p., once daily for 2 weeks
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Result:Significantly enhanced the amplitude of the activity rhythm and the total activity level in mice.
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Animal Model:PER2::LUC gene knock-in mice[1].
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Dosage:10 mg/kg
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Administration:I.p., once, light start time
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Result:Enhanced liver luciferase signaling indicates increased BMAL1 expression.
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Animal Model:Male C57BL/6 mice, 2 months old, were housed under disrupted conditions for 4 weeks, and a ligature was placed around the cervix of the maxillary second molar to establish the murine periodontitis model[1].
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Dosage:10 mg/kg
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Administration:I.p., once daily for 3 weeks
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Result:Significantly reduced alveolar bone resorption (increased bone volume/total volume, reduced bone resorption height).
Reduced inflammatory cell infiltration and osteoclast activity.
Downregulated pro-inflammatory factors (TNF-α, IL-6) and upregulates anti-inflammatory factors (IL-10).
Chemical Information
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No. CAS 3092129-97-7
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Peso molecular 623.42
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Fòrmula C24H22F9NO8
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SMILES
OC[C@H]1O[C@@H](OCOC(C(F)(F)F)(C(F)(F)F)C2=CC=C(NC(C3=CC=C(C(F)(F)F)C=C3)=O)C=C2)[C@H](O)[C@@H](O)[C@H]1O
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Synonyms
Gala-SR1078
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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)
Gala-SR Related Classifications
HY-179514 Related Classifications
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