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SR1078

Cat. No. M5676
SR1078 Structure
Size Price Availability Quantity
5mg USD 81  USD90 In stock
10mg USD 121.5  USD135 In stock
50mg USD 468  USD520 In stock
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Quality Control
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
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 431.25
Formula C17H10F9NO2
CAS Number 1246525-60-9
Purity 99.03%
Solubility 10 mM in DMSO
Storage at -20°C
References

Imiquimod-induced psoriasis-like skin inflammation is suppressed by BET bromodomain inhibitor in mice through RORC/IL-17A pathway modulation.
Nadeem A, et al. Pharmacol Res. 2015 Sep;99:248-57. PMID: 26149470.

Identification of SR1078, a synthetic agonist for the orphan nuclear receptors RORα and RORγ.
Wang Y, et al. ACS Chem Biol. 2010 Nov 19;5(11):1029-34. PMID: 20735016.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SR1078 supplier, ROR, inhibitors

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