Art. -Nr.: HY-101973

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XL041

(Synonyms: BMS-852927)

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XL041 (BMS-852927) is an LXRβ-selective agonist.

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Reinheit: 98.80%
CAS. Nr.: 1256918-39-4
Formel: C₂₉H₂₈Cl₂F₂N₂O₄S
Molecular Weight:609.51

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

XL041 Chemical Structure

CAS. Nr.: 1256918-39-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

XL041 (BMS-852927) is an LXRβ-selective agonist.

IC₅₀ & Target

LXRβ^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CV-1	EC₅₀	24 nM Compound: 15	Agonist activity at human LXR-beta expressed in African green monkey CV1 cells measured after 18 to 20 hrs by luciferase reporter gene assay Agonist activity at human LXR-beta expressed in African green monkey CV1 cells measured after 18 to 20 hrs by luciferase reporter gene assay	[PMID: 27994765]
CV-1	EC₅₀	8 nM Compound: 15	Agonist activity at human LXR-alpha expressed in African green monkey CV1 cells measured after 18 to 20 hrs by luciferase reporter gene assay Agonist activity at human LXR-alpha expressed in African green monkey CV1 cells measured after 18 to 20 hrs by luciferase reporter gene assay	[PMID: 27994765]
CV-1	IC₅₀	69 nM Compound: 15	Antagonist activity at human LXR-alpha expressed in African green monkey CV1 cells measured after 18 to 20 hrs in presence of LXR pan agonist 1-(2,4-difluorobenzyl)-2-oxo-6-(4-phenoxyphenyl)-4-(trifluoromethyl)-1,2-dihydropyridine-3-carbonitrile by lucife Antagonist activity at human LXR-alpha expressed in African green monkey CV1 cells measured after 18 to 20 hrs in presence of LXR pan agonist 1-(2,4-difluorobenzyl)-2-oxo-6-(4-phenoxyphenyl)-4-(trifluoromethyl)-1,2-dihydropyridine-3-carbonitrile by lucife	[PMID: 27994765]
HeLa	EC₅₀	0.6 nM Compound: 15	Agonist activity at LXR-beta in human HeLa cells assessed as induction of ABCA1 by beta-galactosidase/luciferase reporter gene assay Agonist activity at LXR-beta in human HeLa cells assessed as induction of ABCA1 by beta-galactosidase/luciferase reporter gene assay	[PMID: 27994765]
HepG2	EC₅₀	1 μM Compound: 15	Agonist activity at human PXR expressed in human HepG2 cells assessed as induction of CYP3A4 measured after 24 hrs by AlamarBlue dye-based luciferase reporter gene assay Agonist activity at human PXR expressed in human HepG2 cells assessed as induction of CYP3A4 measured after 24 hrs by AlamarBlue dye-based luciferase reporter gene assay	[PMID: 27994765]

In Vitro

XL041 (BMS-852927) is an LXRβ-selective agonist with 20% LXRα and 88% LXRβ activity compared to a full pan agonist in transactivation assays. XL041 is potent, with an EC₅₀=9 nM and 26% activity in an in vitro human whole-blood endogenous target gene activation assay (WBA). BMS-852927 has similar binding affinity to LXRα and LXRβ (19 and 12 nM, respectively)^[1].

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

In Vivo

XL041 (BMS-852927), has a very favorable profile at efficacious doses in cynomolgus monkeys and mice. XL041 pre-treatment of C57BL/6J mice for 7 days results in potent, dose-dependent stimulation of cholesterol efflux in this system, reaching a maximum in the 3 mg/kg/day dose group of 70% above vehicle in the initial efflux rate. Similar results are obtained in LDLR knockout (KO) mice. In a separate study, XL041 inhibits the progression of atherosclerosis in a 12 week study in LDLR KO mice. Importantly, the dose response for inhibition of atherosclerosis (0.1-3 mg/kg/day) is similar to the dose response for macrophage reverse cholesterol transport (RCT) stimulation (0.03-3 mg/kg/day), a major underlying mechanism through which LXR agonists affect the disease^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1256918-39-4
Appearance Solid
Molecular Weight 609.51
Formel C₂₉H₂₈Cl₂F₂N₂O₄S
Color White to off-white
SMILES

OC(C)(C)C1=CN(C2=CC=C(C3=CC(S(=O)(C)=O)=C(CO)C(F)=C3)C=C2F)C(C(C)(C4=C(Cl)C=CC=C4Cl)C)=N1
Synonyms

BMS-852927
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (164.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6407 mL

8.2033 mL

16.4066 mL

5 mM

0.3281 mL

1.6407 mL

3.2813 mL

10 mM

0.1641 mL

0.8203 mL

1.6407 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.10 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

Peritoneal macrophages are prepared from male C57BL/6 mice that are stimulated with 4% thioglycolate for 4 days. Macrophages are cultured in DMEM supplemented with 20% FBS and 100 U/mL antibiotic-antimycotic. Macrophages are incubated with LXR agonists (eg, XL041) in serum-free DMEM for 20hrs, followed by 5hr treatment of LPS (20 ng/mL). The effect of agonists on IL-23α and Mertk mRNAs is determined^[1].

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

Animal Administration^[1]

Mice^[1]
To study effects of LXR agonists on neutrophils, C57BL/6 mice pre-acclimated to oral dosing (n=8/group) are randomly assigned to vehicle; 0.03, 0.1, 1, or 3 mg/kg/day XL041; and 0.3 or 3 mg/kg/day GW3965 and dosed orally for 3 days. Following anesthesia with isoflurane, blood is collected by retro-orbital bleeding and analyzed for neutrophil levels using an Advia hematology instrument employing peroxidase staining.
Monkeys^[1]
All studies are performed in male animals. In a PD study, animals are randomized into six treatment groups (n=3/group) and dosed once daily with vehicle, 10 mg/kg/day T0901317, and 0.1, 0.3, 1, or 3 mg/kg/day XL041 for 14 days. Blood RNA and plasma lipids are determined at baseline and days 1, 4, 7, and 14 of dosing for the pharmacodynamic (PD)study, and on days 1 and 7 for the liver triglyceride (TG) magnetic resonance spectroscopy (MRS) study.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)

Verweise

[1]. Kirchgessner TG, et al. Beneficial and Adverse Effects of an LXR Agonist on Human Lipid and Lipoprotein Metabolism and Circulating Neutrophils. Cell Metab. 2016 Aug 9;24(2):223-33. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6407 mL	8.2033 mL	16.4066 mL	41.0166 mL
	5 mM	0.3281 mL	1.6407 mL	3.2813 mL	8.2033 mL
	10 mM	0.1641 mL	0.8203 mL	1.6407 mL	4.1017 mL
	15 mM	0.1094 mL	0.5469 mL	1.0938 mL	2.7344 mL
	20 mM	0.0820 mL	0.4102 mL	0.8203 mL	2.0508 mL
	25 mM	0.0656 mL	0.3281 mL	0.6563 mL	1.6407 mL
	30 mM	0.0547 mL	0.2734 mL	0.5469 mL	1.3672 mL
	40 mM	0.0410 mL	0.2051 mL	0.4102 mL	1.0254 mL
	50 mM	0.0328 mL	0.1641 mL	0.3281 mL	0.8203 mL
	60 mM	0.0273 mL	0.1367 mL	0.2734 mL	0.6836 mL
	80 mM	0.0205 mL	0.1025 mL	0.2051 mL	0.5127 mL
	100 mM	0.0164 mL	0.0820 mL	0.1641 mL	0.4102 mL

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XL041

Anti-Cardiovascular Disease Compound Library

Lipid Metabolism Compound Library

Targeted Diversity Library

Nuclear Receptor Compound Library

Metabolic Enzyme Compound Library

Highly Selective Activators Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Metabolism/Protease Compound Library

Clinical Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

XL041

Anti-Cardiovascular Disease Compound Library

Lipid Metabolism Compound Library

Targeted Diversity Library

Nuclear Receptor Compound Library

Metabolic Enzyme Compound Library

Highly Selective Activators Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Metabolism/Protease Compound Library

Clinical Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

XL041 Related Classifications

HY-101973 Related Classifications