2. Metabolic Enzyme/Protease
  3. FXR
  4. HEC96719

HEC96719 is a selective and orally active tricyclic farnesoid X receptor (FXR) agonist with EC50 values of 1.37 and 1.55 nM by time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. HEC96719 significantly improves non-alcoholic steatohepatitis (NASH) and liver fibrosis with favorable tissue distribution in liver and intestine. HEC96719 can be used for the research of non-alcoholic steatohepatitis.

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

HEC96719 Chemical Structure

HEC96719 Chemical Structure

CAS No. : 2181834-03-5

Size Price Stock Quantity
1 mg USD 200 In-stock
5 mg USD 500 In-stock
10 mg USD 800 In-stock
25 mg USD 1600 In-stock
50 mg USD 2600 In-stock
100 mg USD 4200 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

HEC96719 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

HEC96719 is a selective and orally active tricyclic farnesoid X receptor (FXR) agonist with EC50 values of 1.37 and 1.55 nM by time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. HEC96719 significantly improves non-alcoholic steatohepatitis (NASH) and liver fibrosis with favorable tissue distribution in liver and intestine. HEC96719 can be used for the research of non-alcoholic steatohepatitis[1].

IC50 & Target

EC50: 1.37 nM (FXR, TR-FRET), 1.55 nM (FXR, luciferase reporter assay)[1].
In Vivo

HEC96719 (0.5, 1.5 and 5 mg/kg; oral administration, once daily for 14 days) shows in vivo efficacy for the activation of FXR by measuring the increasing level of fibroblast growth factor 15 (FGF15)[1].
HEC96719 (5 mg/kg; oral administration, once) increases the level of liver bile salt export pump (BSEP) and ileum FGF15[1].
HEC96719 (0.1, 0.3 and 1 mg/kg; oral administration, once daily for 6 weeks) significantly improves NASH symptoms[1].
HEC96719 (0.1, 0.3 and 1 mg/kg; oral administration, once daily for 4 weeks) shows efficacy for improving liver fibrosis and has better effects than obeticholic acid (OCA)[1].

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

Animal Model: Male ob/ob nonalcoholic steatohepatitis (NASH) mouse models[1]
Dosage: 0.1, 0.3 and 1 mg/kg
Administration: Oral administration; 0.1, 0.3 and 1 mg/kg, once daily for 6 weeks
Result: Decreased levels of serum alanine aminotransferase (ALT) and liver triglyceride (TG), dose-dependently increased NASH activity and reduced NASH activity score.
Animal Model: Male C57BL/6 liver fibrosis mouse models[1]
Dosage: 0.1, 0.3 and 1 mg/kg
Administration: Oral administration; 0.1, 0.3 and 1 mg/kg, once daily for 4 weeks
Result: Decreased levels of serum ALT and TBIL, and reduced fibrosis area.
Clinical Trial
Molecular Weight

549.40

Formula

C29H22Cl2N2O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C2C(OC3=CC=C(OCC4=C(C5CC5)ON=C4C6=C(Cl)C=CC=C6Cl)N=C3C7(CC7)C2)=C1)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (182.02 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 1.8202 mL 9.1008 mL 18.2017 mL
5 mM 0.3640 mL 1.8202 mL 3.6403 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: 5 mg/mL (9.10 mM); Clear solution; Need ultrasonic and warming and heat to 80°C

    This protocol yields a clear solution of 5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: 5 mg/mL (9.10 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 5 mg/mL. 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 (50.0 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

Animal weight
(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 +
% 
+
%
Tween-80 +
%
Saline
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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8202 mL 9.1008 mL 18.2017 mL 45.5042 mL
5 mM 0.3640 mL 1.8202 mL 3.6403 mL 9.1008 mL
10 mM 0.1820 mL 0.9101 mL 1.8202 mL 4.5504 mL
15 mM 0.1213 mL 0.6067 mL 1.2134 mL 3.0336 mL
20 mM 0.0910 mL 0.4550 mL 0.9101 mL 2.2752 mL
25 mM 0.0728 mL 0.3640 mL 0.7281 mL 1.8202 mL
30 mM 0.0607 mL 0.3034 mL 0.6067 mL 1.5168 mL
40 mM 0.0455 mL 0.2275 mL 0.4550 mL 1.1376 mL
50 mM 0.0364 mL 0.1820 mL 0.3640 mL 0.9101 mL
60 mM 0.0303 mL 0.1517 mL 0.3034 mL 0.7584 mL
80 mM 0.0228 mL 0.1138 mL 0.2275 mL 0.5688 mL
100 mM 0.0182 mL 0.0910 mL 0.1820 mL 0.4550 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

HEC96719 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:

HEC967192181834-03-5HEC 96719HEC-96719FXRNR1H4selectivetricyclicNASHliver fibrosisTR-FRETmiceoralOCAInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
HEC96719
Cat. No.:
HY-153114
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.