XL041
Based on 1 Customer Validation
XL041 (BMS-852927) is an LXRβ-selective agonist.
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- Purity: 98.80%
- CAS No.: 1256918-39-4
- 화학식: C29H28Cl2F2N2O4S
- 분자량:609.51
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Biological Activity
LXRβ[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | EC50 |
24 nM
Compound: 15
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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
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[PMID: 27994765] |
| CV-1 | EC50 |
8 nM
Compound: 15
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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
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[PMID: 27994765] |
| CV-1 | IC50 |
69 nM
Compound: 15
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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
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[PMID: 27994765] |
| HeLa | EC50 |
0.6 nM
Compound: 15
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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
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[PMID: 27994765] |
| HepG2 | EC50 |
1 μM
Compound: 15
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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
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[PMID: 27994765] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1256918-39-4
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Appearance Solid
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분자량 609.51
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화학식 C29H28Cl2F2N2O4S
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Color White to off-white
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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
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Synonyms
BMS-852927
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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.
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.
순도&문서
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Data Sheet (279 KB)
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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)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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.
| 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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