LY2562175
Based on 1 Customer Validation
LY2562175 is a potent and selective FXR agonist, with an EC50 of 193 nM.
For research use only. We do not sell to patients.
- Purity: 99.49%
- CAS No.: 1103500-20-4
- Formula: C28H27Cl2N3O4
- Molecular Weight:540.44
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Bioactive Compound Library Max
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Biological Activity
EC50: 193 nM (FXR)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
>10000 nM
Compound: 1; LY2562175
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Agonist activity at glucocorticoid receptor (unknown origin) expressed in HEK293 cells assessed as transcriptional activation
Agonist activity at glucocorticoid receptor (unknown origin) expressed in HEK293 cells assessed as transcriptional activation
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[PMID: 26568144] |
| HEK293 | EC50 |
>10000 nM
Compound: 1; LY2562175
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Agonist activity at mineralocorticoid receptor (unknown origin) expressed in HEK293 cells assessed as transcriptional activation
Agonist activity at mineralocorticoid receptor (unknown origin) expressed in HEK293 cells assessed as transcriptional activation
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[PMID: 26568144] |
| HEK293 | EC50 |
>10000 nM
Compound: 1; LY2562175
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Agonist activity at progesterone receptor (unknown origin) expressed in HEK293 cells assessed as transcriptional activation
Agonist activity at progesterone receptor (unknown origin) expressed in HEK293 cells assessed as transcriptional activation
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[PMID: 26568144] |
| HEK293 | EC50 |
193 nM
Compound: 1; LY2562175
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Agonist activity at human FXR transfected in HEK293 cells assessed as transcriptional activity by luciferase reporter gene assay
Agonist activity at human FXR transfected in HEK293 cells assessed as transcriptional activity by luciferase reporter gene assay
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[PMID: 26568144] |
| HEK293 | EC50 |
>10000 nM
Compound: 1; LY2562175
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Agonist activity at androgen receptor (unknown origin) expressed in HEK293 cells assessed as transcriptional activation
Agonist activity at androgen receptor (unknown origin) expressed in HEK293 cells assessed as transcriptional activation
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[PMID: 26568144] |
LY2562175 promotes transcriptional activation of human FXR in a cell-based co-transfection assay with an EC50 of 193 nM. LY2562175 promotes recruitment of a peptide from the nuclear receptor interaction domain of the coactivator SRC-1 with a relative EC50 of 121 nM and 93.5% efficacy as compare to GW4064[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1103500-20-4
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Appearance Solid
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Molecular Weight 540.44
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Formula C28H27Cl2N3O4
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Color White to light yellow
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SMILES
O=C(C1=CN(C)C2=C1C=CC(N3CCC(OCC4=C(C5CC5)ON=C4C6=C(Cl)C=CC=C6Cl)CC3)=C2)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 62.5 mg/mL (115.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
LY2562175 is tested in concentration-response curves by an FXR-SRC-1 Cofactor Recruitment assay using the Alpha Screen technology according to the manufacturer instructions. Briefly, purified 6-HIS-tagged human FXR ligand-binding domain (amino acids 242-472), purified GST-tagged human SRC-1 nuclear receptor-interacting domain (amino acids 220-394), Nickel Chelate donor beads and Anti-GST antibody acceptor beads are mixed together and 12 μL per well is aliquoted into 384 well plates. Add LY2562175 in 3 μL per well for a total assay volume of 15 μL and incubate at room temperature in the dark for 4 hours. After incubation, LY2562175 that binds FXR and induces the interaction between the FXR and SRC-1 will bring the two bead types into proximity generating luminescence that is quantified using a Packard Fusion instrument. Calculate EC50 values for LY2562175[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
To assess the potency and efficacy of LY2562175 in vivo, studies are conducted in 8 week old, male LDLR null mice fed a “Western” diet. Animals are allowed to acclimate to the high fat/high cholesterol chow TD88137 (containing 0.15% cholesterol and 42% fat) for 2 weeks prior to the study. Animals are divided into groups of six and dosed once daily for 1 week by gavage with solutions of LY2562175 in situ sodium salt or with vehicle (5% Solutol, 5% EtOH, 1 wt %/v CMC) at a dose volume of 5 mL/kg. On the seventh day, animals are bled by cardiac puncture under anesthesia with CO2. Serum is prepared from individual animals for determination of cholesterol and triglycerides by enzymatic analysis. Pooled samples from each treatment group are used for determination of lipoprotein subtypes. ED50 values (dose producing half-maximal effect) for the decrease in serum cholesterol and triglycerides are determined by nonlinear regression analysis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8503 mL | 9.2517 mL | 18.5034 mL | 46.2586 mL |
| 5 mM | 0.3701 mL | 1.8503 mL | 3.7007 mL | 9.2517 mL | |
| 10 mM | 0.1850 mL | 0.9252 mL | 1.8503 mL | 4.6259 mL | |
| 15 mM | 0.1234 mL | 0.6168 mL | 1.2336 mL | 3.0839 mL | |
| 20 mM | 0.0925 mL | 0.4626 mL | 0.9252 mL | 2.3129 mL | |
| 25 mM | 0.0740 mL | 0.3701 mL | 0.7401 mL | 1.8503 mL | |
| 30 mM | 0.0617 mL | 0.3084 mL | 0.6168 mL | 1.5420 mL | |
| 40 mM | 0.0463 mL | 0.2313 mL | 0.4626 mL | 1.1565 mL | |
| 50 mM | 0.0370 mL | 0.1850 mL | 0.3701 mL | 0.9252 mL | |
| 60 mM | 0.0308 mL | 0.1542 mL | 0.3084 mL | 0.7710 mL | |
| 80 mM | 0.0231 mL | 0.1156 mL | 0.2313 mL | 0.5782 mL | |
| 100 mM | 0.0185 mL | 0.0925 mL | 0.1850 mL | 0.4626 mL |
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