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| 10mg |
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| 25mg |
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| 100mg |
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Purity: ≥98%
BMS-852927 (also known as XL041) is a partial agonist of LXRβ (liver X receptor β). BMS-852927 had favorable profiles in animal models with a wide therapeutic index in cynomolgus monkeys and mice. In healthy subjects and hypercholesterolemic patients, reverse cholesterol transport pathways were induced similarly to that in animal models. However, increased plasma and hepatic TG, plasma LDL-C, apoB, apoE, and CETP and decreased circulating neutrophils were also evident. Furthermore, similar increases in LDL-C were observed in normocholesterolemic subjects and statin-treated patients. The primate model markedly underestimated human lipogenic responses and did not predict human neutrophil effects. These studies demonstrate both beneficial and adverse LXR agonist clinical responses and emphasize the importance of further translational research in this area.
| ln Vitro |
In transactivation experiments, XL041 (BMS-852927) demonstrates 20% LXRα and 88% LXRβ activity in comparison to the full pan agonist. With an EC50 of 9 nM and 26% activity in an in vitro human whole blood endogenous target gene activation assay (WBA), XL041 is a very powerful drug. Comparable binding affinities of BMS-852927 for LXRα and LXRβ (19 and 12 nM, respectively) have been reported [1].
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| ln Vivo |
At effective dosages, XL041 (BMS-852927) exhibits very positive characteristics in cynomolgus monkeys and mice. After giving XL041 to C57BL/6J mice for seven days, the system's cholesterol efflux was effectively stimulated in a dosage-dependent manner. The highest efflux rate was observed in the group given a dose of 3 mg/kg/day, which was 70% higher than the vehicle. Mice that were LDLR knockout (KO) had similar outcomes. In a further 12-week trial, XL041 prevented atherosclerosis from progressing in mice lacking the LDLR gene. Significantly, the dose-response for increasing macrophage reverse cholesterol transfer (RCT) (0.03-3 mg/kg/day) and suppressing atherosclerosis (0.1-3 mg/kg/day) was comparable. is a key underlying process by which LXR agonists impact the illness [1].
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| References |
| Molecular Formula |
C29H28CL2F2N2O4S
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|---|---|
| Molecular Weight |
609.511431694031
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| Exact Mass |
608.111
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| CAS # |
1256918-39-4
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| PubChem CID |
49787490
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| Appearance |
White to off-white solid powder
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| LogP |
5.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
40
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| Complexity |
974
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(C1C(=CC=CC=1Cl)Cl)(C1=NC(C(O)(C)C)=CN1C1C=CC(C2C=C(F)C(CO)=C(S(=O)(=O)C)C=2)=CC=1F)(C)C
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| InChi Key |
HNAJDMYOTDNOBK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H28Cl2F2N2O4S/c1-28(2,26-19(30)7-6-8-20(26)31)27-34-25(29(3,4)37)14-35(27)23-10-9-16(11-22(23)33)17-12-21(32)18(15-36)24(13-17)40(5,38)39/h6-14,36-37H,15H2,1-5H3
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| Chemical Name |
2-(2-(2-(2,6-dichlorophenyl)propan-2-yl)-1-(3,3′-difluoro-4′-(hydroxymethyl)-5′-(methylsulfonyl)biphenyl-4-yl)-1H-imidazol-4-yl)propan-2-ol
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| Synonyms |
BMS-852927; BMS 852927; BMS852927; XL041; XL-041; XL 041.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~164.07 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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