LXRβ agonist CL2-57

Chemical Structure : LXRβ agonist CL2-57

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货号: PC-49757Not For Human Use, Lab Use Only.

LXRβ agonist CL2-57 is a non-lipogenic ABCA1 inducer and an LXRβ-selective agonist (EC50=1.3 uM) and PPAR/RXR antagonist.

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生物&药学活性

LXRβ agonist CL2-57 is a non-lipogenic ABCA1 inducer and an LXRβ-selective agonist (EC50=1.3 uM) and PPAR/RXR antagonist.
CL2-57 enhances ABCA1-linked luciferase activity in HepG2 liver cells (Emax=250%; EC50=1.8 uM).
CL2-57 selectively induces ABCA1 and lessens inflammation in vitro, CL2-57 dose-dependently increased cholesterol efflux from macrophages to apoA1, the primary acceptor of cholesterol from ABCA1 in vivo.
CL2-57 (10 mg/kg oral gavage) enhances glucose tolerance and insulin sensitivity in mice fed a high-fat diet (HFD).
CL2-57 reduces HFD-induced adiposity and alterations in liver gene expression, also reduces gluconeogenic metabolite, broadly attenuated pro-inflammatory cytokines, enzymes, and metabolites in HFD mice.

物理化学性质&存储条件

分子量	539.01
分子式	C23H23ClN2O7S2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3-(5-chloro-3-(N-(3,4-diethoxyphenyl)-N-methylsulfamoyl)thiophene-2-carboxamido)benzoic acid

参考文献

1. Cutler T Lewandowski, et al. EBioMedicine. 2021 Apr;66:103287.