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LY2562175

Catalog No. T15806   CAS 1103500-20-4

LY2562175 is an effective and selective FXR agonist (EC50: 193 nM).

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LY2562175 Chemical Structure
LY2562175, CAS 1103500-20-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 163.00
2 mg In stock $ 223.00
5 mg In stock $ 345.00
10 mg In stock $ 547.00
25 mg In stock $ 886.00
50 mg In stock $ 1,190.00
100 mg In stock $ 1,630.00
1 mL * 10 mM (in DMSO) In stock $ 397.00
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Purity: 99.96%
Purity: 99.78%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description LY2562175 is an effective and selective FXR agonist (EC50: 193 nM).
Targets&IC50 FXR:(EC50)193 nM
In vitro LY2562175 boosts transcriptional activation of human FXR in a cell-based co-transfection assay (EC50: 193 nM) and it also promotes the recruitment of a peptide from the nuclear receptor interaction domain of the coactivator SRC-1 (a relative EC50: 121 nM). It has 93.5% efficacy as compare to GW4064.
In vivo LY2562175 induces a dose-dependent decrease in serum cholesterol and serum triglycerides. LY2562175(female ZDF rats) treatment, causes a dose-dependent lowering of plasma triglycerides in the fasted and nonfasted states. LY2562175 further lowers fasted and nonfasted plasma triglycerides when administered as a fixed-dose combination with BRL49653. At a dose of 10 mg/kg, the decrease in cholesterol with LY2562175 is 80% below vehicle-treated animals, and the decrease in serum triglycerides is 76% from the control group. The ED50 for serum cholesterol is determined to be 2 and 3.4 mg/kg for serum triglycerides. FPLC fractionation of the lipoproteins shows that LY2562175 treatment causes a reduction in vLDL-C and a dramatic increase in HDL-c in this animal model.
Molecular Weight 540.44
Formula C28H27Cl2N3O4
CAS No. 1103500-20-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 0.1 mg/mL (insoluble)

DMSO: 62.5 mg/mL (115.65 mM), sonification is recommended.

TargetMolReferences and Literature

1. Genin MJ, et al. Discovery of 6-(4-{[5-Cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl]methoxy}piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic Acid: A Novel FXR Agonist for the Treatment of Dyslipidemia. J Med Chem. 2015 Dec 24;58(24):9768-72.

Related compound libraries

This product is contained In the following compound libraries:
Autophagy Compound Library NO PAINS Compound Library Anti-Metabolism Disease Compound Library Metabolism Compound Library Lipid Metabolism Compound Library Nuclear Receptor Compound Library Bioactive Compound Library Bioactive Compounds Library Max ReFRAME Related Library

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Keywords

LY2562175 1103500-20-4 Autophagy Metabolism FXR NR1H4 Inhibitor LY 2562175 inhibit LY-2562175 inhibitor

 

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