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SR1078

Catalog No. T4594 CAS 1246525-60-9

Synonyms: SR 1078

SR1078 is an agonist of retinoic acid receptor-related orphan receptor (ROR)α/γ.

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SR1078, CAS 1246525-60-9

Pack Size	Availability	Price/USD
1 mg	In stock	$ 35.00
2 mg	In stock	$ 50.00
5 mg	In stock	$ 82.00
10 mg	In stock	$ 117.00
25 mg	In stock	$ 238.00
50 mg	In stock	$ 387.00
100 mg	In stock	$ 575.00
1 mL * 10 mM (in DMSO)	In stock	$ 84.00

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Purity: 98.74%

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Description	SR1078 is an agonist of retinoic acid receptor-related orphan receptor (ROR)α/γ.
In vitro	SR1078 is a synthetic RORα/RORγ ligand. SR1078 modulates the conformation of RORγ in a biochemical assay and activates RORα and RORγ driven transcription. Furthermore, SR1078 stimulates expression of endogenous ROR target genes in HepG2 cells that express both RORα and RORγ. In a cell-based chimeric receptor Gal4 DNA-binding domain-NR ligand binding domain cotransfection assay, SR1078 significantly inhibits the constitutive transactivation activity of RORα and RORγ, but has no effect on the activity of FXR, LXRα and LXRβ. In a RORα cotransfection assay, treatment of cells with SR1078 (10 μM) results in a significant increase in transcription. Similarly, in the RORγ cotransfection assay, SR1078 treatment results in a stimulation of RORγ-dependent transcription activity[1].
In vivo	The pharmacokinetic properties of SR1078 are examined in mice and noted significant exposure. Plasma concentrations reach 3.6 μM 1h after a 10 mg/kg i.p. injection of SR1078 and sustained levels of above 800 nM even 8h after the single injection. These levels are sufficient to perform a proof-of-principle experiment to determine if SR1078 treatment would stimulate ROR target gene expression in an animal model. Mice are treated with SR1078 (10 mg/kg i.p.) and 2h after the injection the livers are harvested and mRNA purified for assessment of?G6Pase?and?FGF21?gene expression.T he expression of both?FGF21?and?G6Pase?is significantly stimulated by SR1078 treatment vs. vehicle control[1].

Synonyms	SR 1078
Molecular Weight	431.25
Formula	C17H10F9NO2
CAS No.	1246525-60-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (104.35 mM)

References and Literature

1. Wang Y, et al. Identification of SR1078, a synthetic agonist for the orphan nuclear receptors RORα and RORγ. ACS Chem Biol. 2010 Nov 19;5(11):1029-34.

Citations

1. Dou X, Huo T, Liu Y, et al.Discovery of novel and selective farnesoid X receptor antagonists through structure-based virtual screening, preliminary structure-activity relationship study, and biological evaluation.European Journal of Medicinal Chemistry.2024: 116323.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Metabolism Disease Compound Library Nuclear Receptor Compound Library Lipid Metabolism Compound Library Bioactive Compounds Library Max Bioactive Compound Library Kinase Inhibitor Library Target-Focused Phenotypic Screening Library NO PAINS Compound Library Metabolism Compound Library

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Keywords

SR1078 1246525-60-9 Metabolism ROR inhibit SR-1078 SR 1078 RAR-related orphan receptor Inhibitor inhibitor

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