2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Cell Cycle/DNA Damage
  3. FXR Cytochrome P450 RAR/RXR PPAR ROR
  4. F44-A13

F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders.

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

F44-A13 Chemical Structure

F44-A13 Chemical Structure

CAS No. : 1338190-14-9

Size Price Stock Quantity
1 mg In-stock
5 mg   Get quote  
10 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

F44-A13 Related Antibodies

Top Publications Citing Use of Products

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

View All RAR/RXR Isoform Specific Products:

View All Isoforms
RXRα RXRβ RXRγ

View All PPAR Isoform Specific Products:

View All Isoforms
PPARα PPARβ/δ PPARγ PPAR PPARδ

View All ROR Isoform Specific Products:

View All Isoforms
RORγ RORα RORβ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders[1].

IC50 & Target

PPARα

 

PPARβ

 

RXR α

 

RXRβ

 

RXRγ

 

RORγ

 

In Vitro

F44-A13 demonstrates high selectivity towards various nuclear receptors, including retinoic acid receptor α/β/γ (RARα/β/γ), retinoid X receptor α/β/γ (RXRα/β/γ), pregnane X receptor (PXR), peroxisome proliferators-activated receptors α/β (PPARα/β), thyroid hormone receptor β (THRβ), and retinoic acid receptor-related orphan receptors γ (RORγ)[1].
F44-A13 (50 μM, 24 h) inhibites FXR transcriptional activity in a dose-dependent manner in the presence of 50 μM CDCA (HY-76847) with an IC50 value of 3.0 μM. F44-A13 is a low-toxicity, highly selective FXR antagonist[1].
F44-A13 (F44-A13: 3, 10, 30 μM; CDCA: 100 μM; 24 hours) can improve cholesterol metabolism and reduce cholesterol activity by inducing the expression of CYP7A1. F44-A13 can decrease the expression level of Shp and Bsep, and increase the expression level of CYP7A1[1].

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

F44-A13 Related Antibodies

Cell Viability Assay[1]

Cell Line: HepG2 , HEK293A cells
Concentration: 100 μM
Incubation Time: 24h
Result: Was not cytotoxic to HepG2 and HEK293A cells

RT-PCR[1]

Cell Line: HepG2 cells
Concentration: F44-A13: 3, 10, 30 μM; CDCA: 100 μM
Incubation Time: 24h
Result: Was able to reverse the regulation of FXR downstream target genes Shp, Bsep and Cyp7a1 by CDCA in a dose-dependent manner.
Decreased the expression level of Shp and Bsep, and increased the expression level of Cyp7a1.
In Vivo

F44-A13 (20, 40 mg/kg; Oral gavage (p.o.) and Intraperitoneal injection (i.p.); 4 days) effectively reduces the levels of TC, TG and LDL-C in a C57BL/6 mice model[1].

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

Animal Model: C57BL/6 mice[1]
Dosage: 20, 40 mg/kg
Administration: Intraperitoneal injection (i.p.) and Oral gavage (p.o.); 4 days
Result: Intraperitoneal injection significantly reduced TC levels by more than 28%, and oral administration significantly reduced TC levels in a dose-dependent manner.
Reduced TG levels by more than 30% at both 20 and 40 mg/kg orally, while intraperitoneal injection did not significantly reduce TG levels.
Oral doses of 20 and 40 mg/kg were effective in reducing LDL-C levels by 12% and 23%, and intraperitoneal injections by 38%.
Molecular Weight

544.71

Formula

C28H40N4O5S
CAS No.
Appearance

Solid

Color

White to light brown

SMILES

CCN(C1=CC(OS(=O)(C2=CC=C(C=C2)NC(C)=O)=O)=C(C=C1)CN(C(NC(C)(C)C)=O)CC3CC3)CC
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 (183.58 mM; ultrasonic and warming and heat to 60°C; 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 1.8358 mL 9.1792 mL 18.3584 mL
5 mM 0.3672 mL 1.8358 mL 3.6717 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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 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

Purity: 96.73%

SDS (393 KB)

COA (256 KB) HNMR (275 KB) LCMS (86 KB)

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, 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 1.8358 mL 9.1792 mL 18.3584 mL 45.8960 mL
5 mM 0.3672 mL 1.8358 mL 3.6717 mL 9.1792 mL
10 mM 0.1836 mL 0.9179 mL 1.8358 mL 4.5896 mL
15 mM 0.1224 mL 0.6119 mL 1.2239 mL 3.0597 mL
20 mM 0.0918 mL 0.4590 mL 0.9179 mL 2.2948 mL
25 mM 0.0734 mL 0.3672 mL 0.7343 mL 1.8358 mL
30 mM 0.0612 mL 0.3060 mL 0.6119 mL 1.5299 mL
40 mM 0.0459 mL 0.2295 mL 0.4590 mL 1.1474 mL
50 mM 0.0367 mL 0.1836 mL 0.3672 mL 0.9179 mL
60 mM 0.0306 mL 0.1530 mL 0.3060 mL 0.7649 mL
80 mM 0.0229 mL 0.1147 mL 0.2295 mL 0.5737 mL
100 mM 0.0184 mL 0.0918 mL 0.1836 mL 0.4590 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.

F44-A13 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:

F44-A131338190-14-9FXRCytochrome P450RAR/RXRPPARRORNR1H4CYPsRetinoic acid receptorsRetinoid X receptorsPeroxisome proliferator-activated receptorsRAR-related orphan receptorP-acetylaminobenzene sulfonate derivativesLipid-lowering activity C57BL/6 miceCYP7A1CDCAInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
F44-A13
Cat. No.:
HY-163436
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

SAFETY DATA SHEET (SDS)

English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB)

Request for HNMR Report

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