5-LO/mPGES1-IN-1
Based on 1 Customer Validation
5-LO/mPGES1-IN-1 (Compound 16) is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LO). IC50 values are 0.3 and 0.4 μM, respectively. 5-LO/mPGES1-IN-1 has anti-inflammatory activity.
For research use only. We do not sell to patients.
- Purity: 99.00%
- CAS No.: 1492060-44-2
- Formula: C25H25ClN4O2S2
- Molecular Weight:513.07
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Storage:Powder -20°C, 3 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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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5-LOX 0.4 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.4 μM
Compound: 13
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Inhibition of mPGES-1 in human A549 cells microsomes assessed as reduction in PGE2 formation by RP-HPLC assay
Inhibition of mPGES-1 in human A549 cells microsomes assessed as reduction in PGE2 formation by RP-HPLC assay
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[PMID: 25037914] |
| A549 | IC50 |
0.4 μM
Compound: 16
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Inhibition of mPGES-1 from human A549 cell microsomal membranes using PGH2 as substrate incubated 15 mins prior to substrate addition measured after 1 min by RP-HPLC analysis
Inhibition of mPGES-1 from human A549 cell microsomal membranes using PGH2 as substrate incubated 15 mins prior to substrate addition measured after 1 min by RP-HPLC analysis
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[PMID: 24171493] |
| COS-7 | EC50 |
1.3 μM
Compound: 13
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Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
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[PMID: 25037914] |
| PMNL | IC50 |
0.2 μM
Compound: 13
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Inhibition of 5-LOX in human PMNL cells assessed as reduction in 5-LOX product formation pre-incubated for 15 mins by HPLC method
Inhibition of 5-LOX in human PMNL cells assessed as reduction in 5-LOX product formation pre-incubated for 15 mins by HPLC method
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[PMID: 25037914] |
| PMNL | IC50 |
0.3 μM
Compound: 13
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Inhibition of 5-LOX in human PMNL cells assessed as reduction in 5-LOX product formation pre-incubated for 15 mins by HPLC based cell-free assay
Inhibition of 5-LOX in human PMNL cells assessed as reduction in 5-LOX product formation pre-incubated for 15 mins by HPLC based cell-free assay
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[PMID: 25037914] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Zymosan-Induced Peritonitis in Mice[1]
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Dosage:10 mg/kg
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Administration:i.p. pretreated 30 minutes before peritonitis induction
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Result:Reduced vascular permeability by 57% and inhibited neutrophil infiltration by 45%.
Chemical Information
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CAS No. 1492060-44-2
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Appearance Solid
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Molecular Weight 513.07
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Formula C25H25ClN4O2S2
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Color White to off-white
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SMILES
O=C(C(CCCCCC)SC1=NC(Cl)=CC(NC2=NC(C3=CC4=C(C=CC=C4)C=C3)=CS2)=N1)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Purity & Documentation
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Data Sheet (267 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
5-LO/mPGES1-IN-1 Related Classifications
HY-126898 Related Classifications
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