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Cat. No.: HY-173393

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LXRα agonist 1

LXRα agonist 1 is a selective LXRα agonist, with EC₅₀ values of 42 nM and 266 nM against purified LXRα and LXRβ, respectively. LXRα agonist 1 acts as a lipotoxicity inducer, triggering the production of toxic saturated fatty acids in tumor cells, and induces lipotoxicity-mediated cancer cell death when combined with the Raf inhibitor Sorafenib (HY-10201). LXRα agonist 1 can be used in the research of hepatocellular carcinoma.

For research use only. We do not sell to patients.

CAS No.: 1790089-97-2
Formula: C₂₈H₂₇N₃O₂
Molecular Weight:437.53

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (277 KB)

LXRα agonist 1 Chemical Structure

CAS No.: 1790089-97-2

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
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Biological Activity

Description

IC₅₀ & Target

^[1]

LXRα

42 nM (EC₅₀)

LXRβ

266 nM (EC₅₀)

In Vitro

Anti-cancerOxidative StressEndoplasmic Reticulum StressOthers

Anti-cancer

LXRα agonist 1 (5 d) alone does not reduce the viability of Hep3B hepatocellular carcinoma cells, but when combined with 2 μM Sorafenib, its EC₅₀ for reducing Hep3B cell viability is 1.7 μM. In contrast, untransformed AML12 and BNL CL.2 hepatocytes exhibit only extremely low sensitivity to this combination regimen^[1].
LXRα agonist 1 (1-5 μM; 5 d) does not reduce the viability of mouse Akt1^Myr; Myc^OE liver cancer organoids, but it exerts significant anti-tumor activity when combined with 4 μM Sorafenib^[1].

Oxidative Stress

LXRα agonist 1 (3 μM; 3 d) alone does not induce significant oxidative stress in Hep3B hepatocellular carcinoma cells, but when combined with 1 μM Sorafenib, it induces strong oxidative stress at a level higher than that induced by the reference LXR agonist^[1].

Oxidative Stress

Endoplasmic Reticulum Stress

LXRα agonist 1 (3 d) combined with 2 μM Sorafenib strongly induces the expression of oxidative stress and endoplasmic reticulum stress response factors including SOD1, GADD34 and CHOP in Hep3B hepatocellular carcinoma cells^[1].

Others

LXRα agonist 1 (Compound 40) (48 h) potently activates LXRα in LXRβ-knockout Hep3B hepatocellular carcinoma cells with an EC₅₀ of 27 nM; in cell-based GFP reporter assays, it exhibits over 23-fold higher selectivity for LXRα over LXRβ (EC₅₀ = 631 nM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Related Protocols :

Chemical Information

CAS No. 1790089-97-2
Molecular Weight 437.53
Formula C₂₈H₂₇N₃O₂
SMILES

O=C(C(C1=CC=CC=C1)=C2NC3=CC=C(N4CCCCC4)C=C3)N(CC5=CC=CC=C5)C2=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Galvez B Pedreira J, et al. Uncovering α-Selectivity for Liver X Receptor Agonists for Lipotoxic Cancer Therapies. Journal of medicinal chemistry. 2025 Apr 10;68(7):7180-7196. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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