sEH-IN-24
sEH-IN-24 is an orally active soluble epoxide hydrolase (sEH) inhibitor with an IC50 of 1.9 nM. sEH-IN-24 inhibits the pro-inflammatory cytokines TNF-α and IL-6. sEH-IN-24 exhibits anti-inflammatory effects and exerts analgesic activity in vivo. sEH-IN-24 prevents pancreatic edema, inflammation and parenchymal atrophy. sEH-IN-24 can be used for the research of acute pancreatitis.
For research use only. We do not sell to patients.
- CAS No.: 3121405-85-1
- Formula: C28H39NO6
- Molecular Weight:485.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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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IL-6 |
sEH 1.9 nM (IC50) |
sEH-IN-24 (Compound (+)-34) (0.46-1000 nM) potently inhibits sEH with an IC50 of 1.9 nM. It forms stable interactions with key active site residues and maintains dynamic stability when forming a complex with this enzyme[1].
sEH-IN-24 exhibits low cytotoxicity against the normal cell lines 293-T, HL7702 and MIHA, with a GI50 value >100 μM[1].
sEH-IN-24 (0.25-8 μM) potently inhibits LPS-induced release of IL-6 and TNF-α in RAW 264.7 and THP-1 macrophages, with IC50 values ranging from 0.7 to 1.3 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
sEH-IN-24 (5-10 mg/kg; p.o.; single dose) demonstrates potent, dose-dependent oral analgesic activity in a mouse acetic acid-induced writhing model, reducing writhing episodes by 45% at the 10 mg/kg dose[1].
sEH-IN-24 (10 mg/kg; i.p.; two doses at 0.5 h and 2.5 h post-first cerulein injection) exerts robust therapeutic activity in a mouse cerulein-induced acute pancreatitis model, reducing pancreatic histopathology scores by 56.3%, lowering pro-inflammatory cytokines, and increasing anti-inflammatory EET/DHET ratios in pancreatic tissue and plasma[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 23−25 g, 6−8 weeks old)[1]
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Dosage:20 mg/kg (p.o.); 10 mg/kg (p.o.); 10 mg/kg (i.p.); 5 mg/kg (i.p.)
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Administration:p.o.; single dose; i.p.; single dose
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Result:Achieved a paw edema inhibition rate of 37.3% at 2 h post-administration, which remained stable at 31.6% 4 h post-peak efficacy.
Increased plasma 8,9-EET/DHET by 219% and 14,15-EET/DHET by 274% relative to the model group, alongside elevations in 8,9-EET (81.1%) and 14,15-EET (108%) levels, and reductions in 8,9-DHET (17.3%) and 14,15-DHET (23.9%) levels at 20 mg/kg (p.o.).
Increased plasma 8,9-EET/DHET by 315%, 11,12-EET/DHET by 198%, and 14,15-EET/DHET by 308% relative to the model group, alongside elevations in 8,9-EET (56.8%), 11,12-EET (60.4%), and 14,15-EET (121%) levels, and reductions in 8,9-DHET (50.0%), 11,12-DHET (18.9%), and 14,15-DHET (28.2%) levels at 10 mg/kg (i.p.).
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Animal Model:C57BL/6J (male, 23−25 g, 6−8 weeks old)[1]
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Dosage:10 mg/kg; 5 mg/kg
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Administration:p.o.; single dose
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Result:Reduced the number of writhing episodes by 45% relative to the model group at 10 mg/kg (p.o.).
Significantly reduced writhing episodes at 5 mg/kg (p.o.), with activity showing a concentration-dependent correlation.
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Animal Model:C57BL/6J (male, 23−25 g, 6−8 weeks old)[1]
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Dosage:10 mg/kg
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Administration:i.p.; two doses at 0.5 h and 2.5 h post-first cerulein injection
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Result:Reduced total pancreatic histopathological scores by 56.3% relative to the model group, alleviating edema, inflammatory infiltration, and parenchymal atrophy.
Reduced plasma TNF-α levels by 46.8% and IL-6 levels by 67.1% relative to the model group.
Increased pancreatic tissue 8,9-EET/DHET by 424%, 11,12-EET/DHET by 1476%, and 14,15-EET/DHET by 2180% relative to the model group.
Increased plasma 11,12-EET/DHET by 86% and 14,15-EET/DHET by 111% relative to the model group.
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Animal Model:C57BL/6J (male, 8 weeks old)[1]
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Dosage:20 mg/kg
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Administration:p.o.; single dose
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Result:Achieved a plasma Cmax of 10,127 ng/mL and AUC0-24h of 148,683 h·ng/mL.
Achieved a liver Cmax of 36,378 ng/g and AUC0-24h of 468,142 h·ng/g.
Achieved a kidney Cmax of 27,061 ng/g and AUC0-24h of 306,849 h·ng/g.
Achieved a brain Cmax of 1021 ng/g and AUC0-24h of 9127 h·ng/g.
Tissue-to-plasma Cmax ratios were 3.59 (liver), 2.67 (kidney), and 0.101 (brain).
Tissue-to-plasma AUC0-24h ratios were 3.15 (liver), 2.06 (kidney), and 0.061 (brain).
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Animal Model:Sprague-Dawley (SD) (male, 200 g)[1]
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Dosage:20 mg/kg (p.o.); 5 mg/kg (i.v.)
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Administration:p.o.; single dose; i.v.; single dose
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Result:After oral administration, had a Tmax of 2.08 h, Cmax of 2064 ng/mL, AUC0-24h of 17834 h·ng/mL, half-life of 2.38 h, volume of distribution of 4017 mL/kg, systemic clearance of 1308 mL/h/kg, and bioavailability of 22.1%.
After intravenous administration, had a Tmax of 0.09 h, Cmax of 7985 ng/mL, AUC0-24h of 20144 h·ng/mL, half-life of 2.21 h, volume of distribution of 896 mL/kg, and systemic clearance of 273 mL/h/kg.
Chemical Information
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CAS No. 3121405-85-1
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Molecular Weight 485.61
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Formula C28H39NO6
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SMILES
CC([C@@H]1C2=C(OC3=C1C(C(C)(C(C3(C)C)=O)C)=O)C=C(C=C2OCCCN4CCOCC4)OC)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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