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BioChemicals
SR9238
tcsc0021352
SR9238
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$
120.00
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ORDERING INFORMATION
International
TAICLONE BIOTECH CORP.
order@taiclone.com
+886-2-2735-9682
+886-2-2735-9807
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Product Description
SR9238 is a synthetic
LXR
antagonist with
IC
50
s of 214 nM and 43 nM for
LXRα
and
LXRβ
, respectively.
IC50 & Target: IC50: 43 nM (LXRβ), 214 nM (LXRα)
[1]
In Vitro:
Results from the cell-based cotransfection assays demonstrate that SR9238 is a synthetic LXR inverse agonist with IC
50
s of 214 nM and 43 nM for LXRα and LXRβ, respectively. SR9238 also effectively suppresses transcription from a fatty acid synthase (
Fasn
) promoter driven luciferase reporter. It is found that 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
[1]
.
In Vivo:
Approximately 6 μM SR9238 is detected in the liver 2h after the injection of SR9238, but no compound is detected in the plasma. SR9238 is also detected in the intestine with either ip or oral administration. SR9238-treated mice display greatly reduced lipid content in the liver. Results demonstrate that both
Tnfa
and
Il1b
expression are substantially reduced (~80% and >95%, respectively) in the SR9238-treated mice when compare to the vehicle-treated mice. 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 (NASH). SR9238 treatment does not alter body weight or percent body fat composition relative to vehicle treated animals during the experiment. Treatment with SR9238 suppresses diet-induced hepatosteatosis, hepatic inflammation, and hepatocellular injury
[1]
.
Information
CAS No
1416153-62-2
Formula
C
31
H
33
NO
7
S
2
Clinical Information
clinicalinformation
Pathway
Metabolic Enzyme/Protease
Target
LXR
Specifications
Purity / Grade
>98%
Solubility
DMSO : 62.5 mg/mL (104.91 mM; Need ultrasonic)
Smiles
smiles
Misc Information
Observed Molecular Weight
595.73
related data
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