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| 25mg |
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Purity: ≥98%
LY2562175 (LY-2562175) is a novel, potent and selective FXR agonist (EC50 = 193 nM) with lipid modulating activity, e.g. lowering LDL and triglycerides while raising HDL in preclinical species. The preclinical ADME properties of LY2562175 were consistent with enabling once daily dosing in humans, and it was ultimately advanced to the clinic for evaluation in humans. LY2562175 promotes transcriptional activation of human FXR in a cell-based cotransfection assay with an EC50 of 193 nM (geometric mean).
| ln Vitro |
In a cell-based co-transfection test, LY2562175 (EC50 = 193 nM) stimulates transcriptional activation of human FXR. In comparison to GW4064, LY2562175 exhibits a 93.5% efficacy in promoting peptide recruitment from the nuclear receptor interaction domain of the coactivator SRC-1, with a relative EC50 of 121 nM [1].
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| ln Vivo |
Serum triglycerides and cholesterol decreased in a dose-dependent manner when treated with LY2562175. LY2562175 lowered serum triglycerides by 76% and cholesterol by 80% at a dose of 10 mg/kg when compared to animals treated with a vehicle. It was found that the ED50 for serum triglycerides was 3.4 mg/kg and the ED50 for serum cholesterol was 2 mg/kg. In both the fasted and non-fasted states, LY2562175 treatment of female ZDF rats led to a dose-dependent reduction in plasma triglycerides. When LY2562175 and BRL49653 were given together at a fixed dosage, the reduction in fasting and non-fasting plasma triglycerides was even greater. In this animal model, FPLC lipoprotein fractionation revealed that LY2562175 treatment led to a significant increase in HDL-c and a decrease in vLDL-C [1].
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| References |
[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
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| Molecular Formula |
C28H27CL2N3O4
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|---|---|
| Molecular Weight |
540.437685251236
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| CAS # |
1103500-20-4
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| Related CAS # |
1103500-20-4 (free acid);LY2502175 sodium;
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| SMILES |
ClC1C=CC=C(C=1C1C(COC2CCN(C3=CC=C4C(C(=O)O)=CN(C)C4=C3)CC2)=C(C2CC2)ON=1)Cl
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| InChi Key |
RPVDFHPBGBMWID-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H27Cl2N3O4/c1-32-14-20(28(34)35)19-8-7-17(13-24(19)32)33-11-9-18(10-12-33)36-15-21-26(31-37-27(21)16-5-6-16)25-22(29)3-2-4-23(25)30/h2-4,7-8,13-14,16,18H,5-6,9-12,15H2,1H3,(H,34,35)
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| Chemical Name |
6-(4-((5-cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl)methoxy)piperidin-1-yl)-1-methyl-1H-indole-3-carboxylic acid
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| Synonyms |
LY 2562175; LY2562175; LY-2562175.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~115.65 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8503 mL | 9.2517 mL | 18.5034 mL | |
| 5 mM | 0.3701 mL | 1.8503 mL | 3.7007 mL | |
| 10 mM | 0.1850 mL | 0.9252 mL | 1.8503 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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