EL244
Based on 1 Customer Validation
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.
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- Purity: 99.55%
- CAS No.: 3047548-70-6
- 화학식: C25H26Cl2N2O5S
- 분자량:537.46
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
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, 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.
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Animal Model:BLM (oropharyngeal aspiration, 0.8 U/Kg)-induced mice[1]
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Dosage:15 mg/Kg
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Administration:Inhaled administration, once daily for 7 days
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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.
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Animal Model:BLM (oropharyngeal aspiration, 0.8 U/Kg)-induced mice[1]
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Dosage:15 mg/Kg
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Administration:Inhaled administration, once daily for 15 days
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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.
Chemical Information
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CAS No. 3047548-70-6
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Appearance Solid
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분자량 537.46
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화학식 C25H26Cl2N2O5S
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Color White to off-white
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SMILES
O=C1NC(C(S1)CC2=CC=C(C=C2)OCCC3CCN(CC3)C(OCC4=CC(Cl)=CC(Cl)=C4)=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (271 KB)
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SDS (252 KB)
- 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)
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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 | 1.8606 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 |
EL244 Related Classifications
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