2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR Phosphodiesterase (PDE)
  4. EL244

EL244 is a dua Autotaxin (ATX) (IC50 = 50 nM) inhibitor and PPARγ (IC50 = 1.3 μM; Kd = 1.3 μM) agonist. EL244 demonstrates low cytotoxicity in human HepG2 cells (EC50 = 81.2 μM) with minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 significantly reduces pulmonary Lysophosphatidic Acid (LPA) levels, attenuates fibrosis, and restores respiratory function with limited systemic absorption in vivo. EL244 can be used for idiopathic pulmonary fibrosis and interstitial lung disease (ILD) research.

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

EL244

EL244 Chemical Structure

CAS No. : 3047548-70-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg   Get quote  
200 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

EL244 Related Antibodies

Top Publications Citing Use of Products

View All PPAR Isoform Specific Products:

View All Isoforms
PPARα PPARβ/δ PPARγ PPAR PPARδ

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

EL244 is a dua Autotaxin (ATX) (IC50 = 50 nM) inhibitor and PPARγ (IC50 = 1.3 μM; Kd = 1.3 μM) agonist. EL244 demonstrates low cytotoxicity in human HepG2 cells (EC50 = 81.2 μM) with minimal inhibition of the cardiac hERG potassium channel (12% at 25 μM). EL244 significantly reduces pulmonary Lysophosphatidic Acid (LPA) levels, attenuates fibrosis, and restores respiratory function with limited systemic absorption in vivo. EL244 can be used for idiopathic pulmonary fibrosis and interstitial lung disease (ILD) research[1].

IC50 & Target[1]

PPAR-γ

1.3 μM (IC50)

Autotaxin

50 nM (IC50)

Parmacokinetics
Species Dose Route Cmax
Mice[1] 30 mg/kg i.p. 40 μM
In Vivo

EL244 (15 mg/kg, 15 mg/kg, once) exhibits favorable lung-targeted pharmacokinetics, characterized by high pulmonary retention, slow local clearance, and limited systemic absorption in the BLM (Bleomycin) (HY-108345) (oropharyngeal aspiration, 0.8 U/Kg)-induced mice model of pulmonary fibrosis[1].
EL244 (15 mg/kg, inhaled administration, once daily for 15 days) post and before BLM administration has anti-fibrotic prophylactic effects in the BLM (oropharyngeal aspiration, 0.8 U/Kg)-induced model of pulmonary fibrosis in the BLM (oropharyngeal aspiration, 0.8 U/Kg)-induced mice model of pulmonary fibrosis[1].
EL244 (30 mg/kg, i.p., once) demonstrates favorable pharmacokinetics, achieving a plasma concentration of 40 μM within 1 hour, maintaining levels around 35 μM for up to 3 hours, and remaining detectable at approximately 15 μM even 9 hours post-dose, with its maximal pharmacodynamic effect coinciding at the 3-hour time point in the BLM (oropharyngeal aspiration, 0.8 U/Kg)-induced mice model of pulmonary fibrosis[1].

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

Animal Model: BLM (oropharyngeal aspiration, 0.8 U/Kg)-induced mice[1]
Dosage: 15 mg/Kg
Administration: Inhaled administration, once daily for 7 days
Result: Diminished inflammation, Appeared fibrotic regions.
Restored all assessed respiratory functions and reduced vascular permeability.
Demonstrated strong anti-fibrotic effects, significantly reducing soluble collagen in BALF and Col1a1 expression in lung tissue.
Reduced collagen deposition and fewer and smaller fibrotic regions.
Animal Model: BLM (oropharyngeal aspiration, 0.8 U/Kg)-induced mice[1]
Dosage: 15 mg/Kg
Administration: Inhaled administration, once daily for 15 days
Result: Improved respiratory functions.
Reduced BLM-induced pulmonary oedema and inflammation.
Reduced Soluble collagen levels in BALF and Col1a1 mrna expression in lung tissue.
Attenuated collagen deposition and the reduction of fibrotic regions.
Not caused any appreciable toxicity in the liver, as indicated by the ALT/AST levels.
Molecular Weight

537.46

Formula

C25H26Cl2N2O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC(C(S1)CC2=CC=C(C=C2)OCCC3CCN(CC3)C(OCC4=CC(Cl)=CC(Cl)=C4)=O)=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 (186.06 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 1.8606 mL 9.3030 mL 18.6060 mL
5 mM 0.3721 mL 1.8606 mL 3.7212 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 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.
Calculation results:
Working solution concentration: mg/mL
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 1.8606 mL 9.3030 mL 18.6060 mL 46.5151 mL
5 mM 0.3721 mL 1.8606 mL 3.7212 mL 9.3030 mL
10 mM 0.1861 mL 0.9303 mL 1.8606 mL 4.6515 mL
15 mM 0.1240 mL 0.6202 mL 1.2404 mL 3.1010 mL
20 mM 0.0930 mL 0.4652 mL 0.9303 mL 2.3258 mL
25 mM 0.0744 mL 0.3721 mL 0.7442 mL 1.8606 mL
30 mM 0.0620 mL 0.3101 mL 0.6202 mL 1.5505 mL
40 mM 0.0465 mL 0.2326 mL 0.4652 mL 1.1629 mL
50 mM 0.0372 mL 0.1861 mL 0.3721 mL 0.9303 mL
60 mM 0.0310 mL 0.1551 mL 0.3101 mL 0.7753 mL
80 mM 0.0233 mL 0.1163 mL 0.2326 mL 0.5814 mL
100 mM 0.0186 mL 0.0930 mL 0.1861 mL 0.4652 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.

EL244 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:

EL2443047548-70-6EL 244EL-244PPARPhosphodiesterase (PDE)Peroxisome proliferator-activated receptorsATXPPARγhuman HepG2 cellspotassium channelidiopathic pulmonary fibrosisInhibitorinhibitorinhibit

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:
EL244
Cat. No.:
HY-179580
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 (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB) Italian - IT (252 KB) Korean - KR (252 KB) Portuguese - PT (252 KB)

Request for HNMR Report

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