SR9238 induces increased interaction of CoRNR box peptides derived from NCoR (NCoR ID1 and NCoR ID2) with both LXRα and LXRβ, while causing decreased interaction with a coactivator NR box peptide derived from TRAP220. SR9238-induced recruitment of CoRNR box peptides is dose-dependent for both LXRα and LXRβ. HepG2 cells treated with SR9238 result in a significant decrease in Fasn and Srebp1c mRNA expression.
SR9238-treated mice display greatly reduced lipid content in the liver. SR9238-treated DIO mice display considerably lower intensity of F4/80 staining versus vehicle-treated DIO mice consistent with a beneficial effect of SR9238 on non-alcoholic steatohepatitis.
Molecular Weight | 595.73 |
Formula | C31H33NO7S2 |
CAS Number | 1416153-62-2 |
Solubility (25°C) | DMSO ≥ 25 mg/mL |
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 Liver X Receptor Products |
---|
BMS-779788
BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ. |
RGX-104 hydrochloride
RGX-104 hydrochloride is a small-molecule LXR (liver X receptor) agonist that modulates innate immunity via transcriptional activation of the ApoE gene. |
Iristectorigenin B
Iristectorigenin B is a liver X receptor (LXR) modulator, which stimulates the transcriptional activity of both LXR-α and LXR-β. |
RGX-104
RGX-104, also known as SB 742881, is a liver X receptor beta (LXR) agonist with potential immunomodulating and antineoplastic activities. |
Yamogenin
Yamogenin (Diosgenin) antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.