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SR1078

Cat. No. M5676
SR1078 Structure
Size Price Availability Quantity
5mg USD 90  USD90 In stock
10mg USD 135  USD135 In stock
50mg USD 520  USD520 In stock
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Quality Control & Documentation
Biological Activity

SR1078 is a newly described synthetic RORα/γ agonist. Treatment of cancer cells with SR1078 leads to p53 stabilization and induction of apoptosis. 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. Pharmacokinetic studies indicate that SR1078 displays reasonable exposure following injection into mice, and consistent with SR1078 functioning as a RORα/RORγ agonist, expression of two ROR target genes, glucose-6-phosphatase and fibroblast growth factor 21, were stimulated in the liver. Thus, SR1078 can be utilized as a chemical tool to probe the function of these receptors both in vitro and in vivo.

Protocol (for reference only)
Cell Experiment
Cell lines HepG2 cells
Preparation method 16 h post-transfection, the cells were treated with vehicle or compound. 24 h post-treatment, the luciferase activity was measured using the Dual-GloTM luciferase assay system.
Concentrations 10 μM
Incubation time 24 h
Animal Experiment
Animal models C57BL6 mice
Formulation
Dosages 10 mg/kg
Administration i.p.
Chemical Information
Molecular Weight 431.25
Formula C17H10F9NO2
CAS Number 1246525-60-9
Solubility (25°C) 10 mM in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Nadeem A, et al. Pharmacol Res. Imiquimod-induced psoriasis-like skin inflammation is suppressed by BET bromodomain inhibitor in mice through RORC/IL-17A pathway modulation.

[2] Wang Y, et al. ACS Chem Biol. Identification of SR1078, a synthetic agonist for the orphan nuclear receptors RORα and RORγ.

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  Catalog
Abmole Inhibitor Catalog




Keywords: SR1078 supplier, ROR, inhibitors, activators


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