LXRalpha/beta AgonistA specific liver X receptor (LXR) dual agonist

LXRα/β Agonist (CAS 264206-85-1)

LXRα/β Agonist is rated 5.0 out of 5 by 1.
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Synonym: GSK 3987
Application: A specific liver X receptor (LXR) dual agonist
CAS Number: 264206-85-1
Purity: ≥98%
Molecular Weight: 384.4
Molecular Formula: C24H20N2O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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LXRα/β Agonist is a cell-permeable maleimide analog which acts as a potent and specific LXR (liver X receptor) dual agonist (EC50= 50 nM and 40 nM for the recruitment of SRC1 to LXRα and LXRβ, respectively). It displays >50-fold selectivity for LXR over a panel of nuclear receptors, which include FXR, PPARα/γ/δ, PXR, AR, ERα/β, GR, and PR. This upregulates ABCA1-dependent transcriptional activity (EC50 = 80 nM) as well as inhibits LPS-stimulated secretion of the proinflammatory cytokine, IL-6, in THP-1 cells.


References

Jaye, M.C., et al. 2005. J. Med. Chem. 48, 5419.

Physical State :
Solid
Solubility :
Soluble in DMSO (200 mg/ml), and methanol (100 mg/ml).
Storage :
Store at 4° C
Melting Point :
264.16° C (Predicted)
Boiling Point :
572.35° C at 760 mmHg (Predicted)
Density :
1.31 g/cm3 (Predicted)
Refractive Index :
n20D 1.68 (Predicted)
IC50 :
LXRβ: EC5050 = 40 nM (human); LXRα: EC5050 = 50 nM (human); GSK-3β: IC50 = >5 µM (human)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
5288679
SMILES :
COC1=CC=C(C=C1)NC2=C(C(=O)N(C2=O)CC3=CC=CC=C3)C4=CC=CC=C4

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Certificate of Analysis

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Rated 5 out of 5 by from An increase in SREBP An increase in SREBP-1 protein expression was observed by WB when comparing untreated Hep G2 cells with those that have been treated with LXR / Agonist. -SCBT QC
Date published: 2015-02-08
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