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.
|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.|
|Incubation time||24 h|
|Animal models||30 week old Diet induced obese (DIO) C57BL/6 male mice|
|Formulation||65% Kcal high-fat diet|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||10 mM in DMSO|
The retinoid-related orphan receptor alpha is essential for the end-stage effector phase of experimental epidermolysis bullosa acquisita.
Sadeghi H, et al. J Pathol. 2015 Sep;237(1):111-22. PMID: 25953430.
Identification of SR3335 (ML-176): a synthetic RORα selective inverse agonist.
Kumar N, et al. ACS Chem Biol. 2011 Mar 18;6(3):218-22. PMID: 21090593.
|Related ROR Products|
S18-000003 is a potent, effective and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt), with an IC50 of 29 nM.
Neoruscogenin is a bioavailable, potent, and high-affinity agonist of the nuclear receptor RORα (NR1F1).
Vimirogant (also known as AGN-242428 and VTP-43742) is a potent, selective and orally active RORγt inhibitor.
GSK805 is a potent, orally bioavailable RORγγ Inhibitor, with pIC50 of 8.4 and >8.2 for RORγ FRET assay and Th17 assay.
SR2211 is a synthetic RORγ-selective modulator, functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM.
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