Art. -Nr.: HY-103704

LY2562175

Name: LY2562175
Brand: MedChemExpress
SKU: HY-103704
Price: 130.00 USD
Availability: InStock
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LY2562175 is a potent and selective FXR agonist, with an EC₅₀ of 193 nM.

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Reinheit : 99.49%
CAS. Nr.: 1103500-20-4
Formel: C₂₈H₂₇Cl₂N₃O₄
Molecular Weight:540.44

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

LY2562175 Chemical Structure

CAS. Nr.: 1103500-20-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target

EC50: 193 nM (FXR)

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	>10000 nM Compound: 1; LY2562175	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	[PMID: 26568144]
HEK293	EC₅₀	>10000 nM Compound: 1; LY2562175	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	[PMID: 26568144]
HEK293	EC₅₀	>10000 nM Compound: 1; LY2562175	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	[PMID: 26568144]
HEK293	EC₅₀	193 nM Compound: 1; LY2562175	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	[PMID: 26568144]
HEK293	EC₅₀	>10000 nM Compound: 1; LY2562175	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	[PMID: 26568144]

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. .

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.

Chemical Information

CAS. Nr. 1103500-20-4
Appearance Solid
Molecular Weight 540.44
Formel C₂₈H₂₇Cl₂N₃O₄
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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