2. Metabolic Enzyme/Protease Autophagy
  3. FXR Autophagy
  4. LY2562175

LY2562175 est un agoniste de FXR qui est puissant et sélectif, avec un EC50 de 193 nM.

LY2562175 is a potent and selective FXR agonist, with an EC50 of 193 nM.

For research use only. We do not sell to patients.

LY2562175 Chemical Structure

LY2562175 Chemical Structure

CAS No. : 1103500-20-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 345 In-stock
Solution
10 mM * 1 mL in DMSO USD 345 In-stock
Solid
1 mg USD 130 In-stock
5 mg USD 290 In-stock
10 mg USD 470 In-stock
25 mg USD 940 In-stock
50 mg USD 1500 In-stock
100 mg USD 2300 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

LY2562175 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

LY2562175 is a potent and selective FXR agonist, with an EC50 of 193 nM[1].

IC50 & Target

EC50: 193 nM (FXR)
In Vitro

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.

LY2562175 Related Antibodies
In Vivo

LY2562175 causes a dose-dependent decrease in serum cholesterol and serum triglycerides. 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 control group. The ED50 for serum cholesterol is determined to be 2 and 3.4 mg/kg for serum triglycerides. Treatment of female ZDF rats with LY2562175 results in a dose dependent lowering of plasma triglycerides in the fasted and nonfasted states. When administered as a fixed dose combination with BRL49653, LY2562175 further lowers fasted and nonfasted plasma triglycerides. FPLC fractionation of the lipoproteins reveals that LY2562175 treatment results in a reduction in vLDL-C and a dramatic increase in HDL-c in this animal model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

540.44

Formula

C28H27Cl2N3O4
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=CN(C)C2=C1C=CC(N3CCC(OCC4=C(C5CC5)ON=C4C6=C(Cl)C=CC=C6Cl)CC3)=C2)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.85 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.49%

COA (252 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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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LY2562175 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LY25621751103500-20-4LY 2562175LY-2562175FXRAutophagyNR1H4Inhibitorinhibitorinhibit

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