sEH-IN-21
sEH-IN-21 is an orally active sEH inhibitor with IC50s of 0.1 nM for hsEH and msEH. sEH-IN-21 potently inhibits NF-κB signaling pathways. sEH-IN-21 shows a strong anti-inflammatory activity, decreases the release of IL-6 and TNF-α and maintained the integrity of the intestinal barrier. sEH-IN-21 can be used for the study of inflammatory bowel disease (IBD).
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- CAS. Nr.: 3084814-46-7
- Formel: C30H40N4O5S
- Molecular Weight:568.73
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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NF-κB |
IL-6 |
hSEH 0.1 nM (IC50) |
mSEH 0.1 nM (IC50) |
sEH-IN-21 (Compound A1) has moderate metabolic stability in rat liver microsomes, with a half-life of 13.51 min and a plasma protein binding rate of 96.2%. [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Tmax | Cmax | T1/2 | CL | Vz | AUC0-∞ | F |
|---|---|---|---|---|---|---|---|---|---|
| Rat | 10 mg/kg | i.v. | 0.03 h | 69.22 μM | 1.03 h | 1.14 L/h | 1.70 L | 8.84 μM·h | 10.25 % |
| Rat | 50 mg/kg | i.g. | 4 h | 0.81 μM | 3.29 h | 11.41 L/h | 55.0 L | 4.53 μM·h | / |
sEH-IN-21 (1 g/kg, i.g., for 7 days) is well tolerated and has an excellent margin of safety in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DSS-induced acute enteritis model established in male C57BL/6J mice (six-week-old).[1]
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Dosage:25, 50, 100 mg/kg
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Administration:Oral gavage (p.o.), for 10 days
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Result:Significantly alleviated the weight loss of mice.
Recovered the length of the colon.
Significantly reduced the histopathology of ulcerative colitis.
Increased the levels of NF-κB, TNF-α and IL-6.
Increased the expression of occludin and claudin.
Chemical Information
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CAS. Nr. 3084814-46-7
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Molecular Weight 568.73
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Formel C30H40N4O5S
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SMILES
O=C1C(N[C@@H]2CC[C@@H](NC(N[C@]3(C4)C[C@H](C5)C[C@]4(C)C[C@@]5(C)C3)=O)CC2)=C(NS(C6=CC=C(C)C=C6)(=O)=O)C1=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
sEH-IN-21 Related Classifications
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