XL041 (BMS-852927) is an agonist of LXRβ-selective.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | 6-8 weeks | $ 127 | |
2 mg | 6-8 weeks | $ 241 | |
4 mg | 6-8 weeks | $ 361 | |
10 mg | 6-8 weeks | $ 571 | |
20 mg | 6-8 weeks | $ 896 |
Description | XL041 (BMS-852927) is an agonist of LXRβ-selective. |
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. BMS-852927 has similar binding affinity to LXRα and LXRβ (19 and 12 nM, respectively). XL041 is potent, with an EC50=9 nM and 26% activity in an in vitro human whole-blood endogenous target gene activation assay (WBA). |
In vivo | XL041 (BMS-852927) which has a very favorable profile at efficacious doses in cynomolgus monkeys and mice. In a separate study, XL041 inhibits the progression of atherosclerosis in a 12 week study in LDLR KO 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. 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. |
Synonyms | BMS-852927 |
CAS No. | 1256918-39-4 |
Chemical Formula | C29H28Cl2F2N2O4S |
Molecular Weight | 609.51 |
Solubility | DMSO: 100 mg/mL (164.07 mM), Need ultrasonic |
Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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