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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | Inquiry | 8-10 weeks | 8-10 weeks | |
| 25 mg | Inquiry | 8-10 weeks | 8-10 weeks | |
| 50 mg | Inquiry | 8-10 weeks | 8-10 weeks | |
| 100 mg | Inquiry | 8-10 weeks | 8-10 weeks | |
| 1 mL x 10 mM (in DMSO) | Inquiry | 8-10 weeks | 8-10 weeks |
| Description | XL041 (BMS-852927) is an agonist selective for LXRβ. |
| In vitro | XL041 (BMS-852927) functions as an LXRβ-selective agonist, exhibiting 20% activity towards LXRα and 88% towards LXRβ relative to a comprehensive pan agonist in transactivation assays. Despite similar binding affinities to LXRα and LXRβ (19 and 12 nM, respectively)[1], XL041 proves to be potent, with an EC50 of 9 nM and achieves 26% activity in an in vitro human whole-blood endogenous target gene activation assay (WBA). |
| In vivo | XL041 (BMS-852927) exhibits a highly favorable efficacy profile at therapeutic doses in both cynomolgus monkeys and mice. In a distinct study, the compound effectively inhibited the progression of atherosclerosis over a 12-week period in LDLR knockout (KO) mice. Additionally, pre-treating C57BL/6J mice with XL041 for seven days induced a potent and dose-dependent increase in cholesterol efflux, peaking at a 70% enhancement over the control with a dose of 3 mg/kg/day. This effect was also observed in LDLR KO mice. Notably, the dosage range that inhibits atherosclerosis (0.1-3 mg/kg/day) aligns closely with the dosage range that stimulates macrophage reverse cholesterol transport (RCT) (0.03-3 mg/kg/day), indicating a conserved mechanism of action for LXR agonists in mitigating the disease. |
| Synonyms | BMS-852927 |
| Molecular Weight | 609.51 |
| Formula | C29H28Cl2F2N2O4S |
| Cas No. | 1256918-39-4 |
| Relative Density. | 1.36 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (164.07 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (5.41 mM), Sonication is recommeded. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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