XL-652
XL-652 Basic information
- Product Name:
- XL-652
- Synonyms:
-
- XL-652
- XL-652,BMS 779788
- BMS-779788
- BMS-779788(XL-652)
- BMS 788
- BMS-779788; BMS 779788; BMS779788; BMS-788; BMS 788; BMS788; XL-652; XL652; XL652; EXEL 04286652; EXEL04286652; EXEL-04286652
- BMS788
- BMS-788
- CAS:
- 918348-67-1
- MF:
- C28H29ClN2O3S
- MW:
- 509.06
- Mol File:
- 918348-67-1.mol
XL-652 Chemical Properties
- Boiling point:
- 738.7±70.0 °C(Predicted)
- Density
- 1.21±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:65.0(Max Conc. mg/mL);127.69(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);58.93(Max Conc. mM)
Ethanol:30.0(Max Conc. mg/mL);58.93(Max Conc. mM) - form
- A crystalline solid
- pka
- 13.56±0.29(Predicted)
- color
- White to off-white
XL-652 Usage And Synthesis
Uses
BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.
in vivo
BMS-779788 induces LXR target genes in blood in vivo with an EC50=610 nM, a value similar to its in vitro blood gene induction potency. BMS-779788 is 29- and 12-fold less potent than the full agonist T0901317 in elevating plasma triglyceride and LDL cholesterol, respectively, with similar results for plasma cholesteryl ester transfer protein and apolipoprotein B[1]. In mice BMS-779788 displays peripheral induction of ABCA1 at 3 and 10 mpk doses with no significant elevation of plasma or hepatic triglycerides at these doses, showing an improved profile compared to a full pan-agonist[2].
References
[1] Kirchgessner TG, et al. Pharmacological characterization of a novel liver X receptor agonist with partial LXRα activity and a favorable window in nonhuman primates. J Pharmacol Exp Ther. 2015 Feb;352(2):305-14. DOI:10.1124/jpet.114.219923
[2] Kick E, et al. Liver X receptor (LXR) partial agonists: biaryl pyrazoles and imidazoles displaying a preference for LXRβ. Bioorg Med Chem Lett. 2015 Jan 15;25(2):372-7. DOI:10.1016/j.bmcl.2014.11.029
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