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Abequolixron (RGX-104) Liver X Receptor agonist

Name: Abequolixron (RGX-104)
Brand: Selleck Chemicals
SKU: S8689
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8689

Abequolixron (RGX-104) is an orally bioavailable liver X receptor agonist that modulates innate immunity via transcriptional activation of the ApoE gene.

Chemical Structure

Molecular Weight: 632.54

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other Liver X Receptor Inhibitors	GW3965 Hydrochloride T0901317 LXR-623 (WAY-252623) SR9243 AZ876 Desmosterol GSK3987 GSK2033

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (158.09 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	12.500mg/ml (19.76mM)	Taking the 1 mL working solution as an example, add 50 μL of 250 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	632.54	Formula	C₃₄H₃₄Cl₂F₃NO₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	610318-03-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(CCOC1=CC=CC(=C1)CC(=O)O)N(CC2=C(C(=CC=C2)C(F)(F)F)Cl)CC(C3=CC=CC=C3)C4=CC=CC=C4.Cl

Mechanism of Action

Targets/IC₅₀/Ki	LXR
In vitro	Abequolixron (RGX-104) is an oral first-in-class LXR agonist that robustly induces ApoE expression, resulting in innate-immune mediated anti-tumor activity. It drives anti-tumor immunity by regulating the abundance and activity of myeloid derived suppressor cells (MDSC) and dendritic cells (DC).
In vivo	Abequolixron (RGX-104) has demonstrated antitumor activity as a monotherapy in several syngeneic and xenograft tumor models, including melanoma, lung cancer, ovarian cancer, GBM and others. Its anti-tumor activity is related to constitutive upregulation of ApoE expression.
References	[1] https://meetinglibrary.asco.org/record/159200/abstract

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