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SR3335

Cat. No. M5675
SR3335 Structure
Synonym:

ML 176

Size Price Availability Quantity
5mg USD 90  USD90 In stock
10mg USD 160  USD160 In stock
50mg USD 580  USD580 In stock
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Quality Control & Documentation
Biological Activity

SR3335 suppresses the expression of endogenous RORα target genes in HepG2 involved in hepatic gluconeogenesis including glucose-6-phosphatase and phosphoenolpyruvate carboxykinase. The first selective synthetic RORα inverse agonists may hold utility for suppression of elevated hepatic glucose production in type 2 diabetics.

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
Incubation time 24 h
Animal Experiment
Animal models 30 week old Diet induced obese (DIO) C57BL/6 male mice
Formulation 65% Kcal high-fat diet
Dosages 15 mg/kg
Administration i.p.
Chemical Information
Molecular Weight 405.34
Formula C13H9F6NO3S2
CAS Number 293753-05-6
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] Sadeghi H, et al. J Pathol. The retinoid-related orphan receptor alpha is essential for the end-stage effector phase of experimental epidermolysis bullosa acquisita.

[2] Kumar N, et al. ACS Chem Biol. Identification of SR3335 (ML-176): a synthetic RORα selective inverse agonist.

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  Catalog
Abmole Inhibitor Catalog




Keywords: SR3335, ML 176 supplier, ROR, inhibitors, activators


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