2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. ROR
  4. 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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Gala-SR

Gala-SR Chemical Structure

CAS No. : 3092129-97-7

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Gala-SR Related Antibodies

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Description

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[1].

IC50 & Target

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.

Gala-SR Related Antibodies

Real Time qPCR[1]

Cell Line: HepG2 cells
Concentration: 5 μM
Incubation Time: 24 h
Result: Upregulated the mRNA expression of G6Pase and FGF21, direct target genes of RORα/γ, in HepG2 cells.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC MRTINF_obs
Mice[1] 10 mg/kg i.p. 3.43 h 0.5 h 1313.1 ng/mL 6077.31 ng·h/mL 4.5 h
Mice[1] 10 mg/kg i.v. 2.49 h 0.5 h 4992.46 ng/mL 8176.18 ng·h/mL 2.97 h
In Vivo

Gala-SR (10 mg/kg, 1 h before light off, i.p., once daily for 2 weeks) significantly enhances the amplitude of activity rhythm and total activity in mice[1].
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.

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].
Dosage: 10 mg/kg
Administration: 1 hour before the end of the light exposure, i.p., once daily for 2 weeks
Result: Significantly enhanced the amplitude of the activity rhythm and the total activity level in mice.
Animal Model: PER2::LUC gene knock-in mice[1].
Dosage: 10 mg/kg
Administration: I.p., once, light start time
Result: Enhanced liver luciferase signaling indicates increased BMAL1 expression.
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].
Dosage: 10 mg/kg
Administration: I.p., once daily for 3 weeks
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).
Molecular Weight

623.42

Formula

C24H22F9NO8
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Gala-SR Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Gala-SR3092129-97-7Gala-SR1078RORRAR-related orphan receptorCircadian rhythmRORα agonistBone lossPeriodontitisInhibitorinhibitorinhibit

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