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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $106 | In Stock | In Stock | |
| 5 mg | $239 | In Stock | In Stock | |
| 10 mg | $388 | In Stock | In Stock | |
| 25 mg | $778 | In Stock | In Stock | |
| 50 mg | $1,230 | In Stock | In Stock | |
| 100 mg | $1,650 | In Stock | In Stock | |
| 200 mg | $2,230 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $283 | In Stock | In Stock |
| 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 |
| Smiles | Cn1cc(C(O)=O)c2ccc(cc12)N1CCC(CC1)OCc1c(onc1-c1c(Cl)cccc1Cl)C1CC1 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: < 0.1 mg/mL (insoluble) DMSO: 62.5 mg/mL (115.65 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.7 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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