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 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. |
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 |
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.
Related ROR Products |
---|
JTE-151
JTE-151 is a RORγ inhibitor that suppresses overactive immune responses by inhibiting RORγ associated with Th17 cell activation.JTE-151 can be used in studies related to autoimmune diseases. |
SAR-441169
SAR-441169 is a RORγt inverse agonist that can be used in studies related to psoriasis. |
GRC-39815
GRC-39815 is a RORγt inverse agonist that can be used in studies related to chronic obstructive pulmonary disease. |
RORγ antagonist 1
RORγ antagonist 1, a potent betulinic acid derivative, is an antagonist of RORγ (KD=0.18 μM). |
RORγt inverse agonist 31
RORγt inverse agonist 31 (14g) is a potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist, with an IC50 of 0.428 μM. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.