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918348-67-1

918348-67-1 structure
918348-67-1 structure
  • Name: BMS-779788
  • Chemical Name: BMS-779788
  • CAS Number: 918348-67-1
  • Molecular Formula: C28H29ClN2O3S
  • Molecular Weight: 509.060
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease LXR
  • Create Date: 2018-04-04 17:30:43
  • Modify Date: 2024-01-02 19:52:34
  • BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.
Name BMS-779788
Synonyms 1H-Imidazole-4-methanol, 2-[1-(2-chlorophenyl)-1-methylethyl]-α,α-dimethyl-1-[3'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]-
2-{2-[2-(2-Chlorophenyl)propan-2-Yl]-1-[3'-(Methylsulfonyl)biphenyl-4-Yl]-1h-Imidazol-4-Yl}propan-2-Ol
2-{2-[2-(2-Chlorophenyl)-2-propanyl]-1-[3'-(methylsulfonyl)-4-biphenylyl]-1H-imidazol-4-yl}-2-propanol
Description BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.
Related Catalog
Target

IC50: 68 nM (LXRα); 14 nM (LXRβ)[1]
In Vitro The LXR selective partial agonist BMS-779788 is identified with potent induction of ATP binding transporters ABCA1 and ABCG1 in human whole blood (EC50=1.2 μM, 55% efficacy)[2].
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].
Animal Admin Monkeys: Male cynomolgus monkeys are used in the study. For a single-dose pharmacokinetic (PK)-pharmacodynamic (PD) study, 2 animals each are treated either with vehicle [0.5% carboxymethyl cellulose and 2% Tween 80 in purified water) or 1 mg/kg BMS-779788. For the 7 day PD study, 18 animals are randomized into 6 treatment groups (N=3/group; 3-6 kg) and received the following treatments at 7 AM daily for 7 days by oral gavage: vehicle, 10 mg/kg per day T0901317 and 0.3, 1, 3, or 10 mg/kg per day BMS-779788[1].
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.

[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.
Density 1.2±0.1 g/cm3
Boiling Point 738.7±70.0 °C at 760 mmHg
Molecular Formula C28H29ClN2O3S
Molecular Weight 509.060
Flash Point 400.6±35.7 °C
Exact Mass 508.158752
LogP 4.85
Appearance light yellow solid
Vapour Pressure 0.0±2.6 mmHg at 25°C
Index of Refraction 1.605
Storage condition -20℃

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title: CAS No. 918348-67-1 | Chemsrc address: https://www.chemsrc.com/en/baike/1470494.html

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