NPC-18915 free base
NPC-18915 free base is a neutrophil activation inhibitor. NPC-18915 free base inhibits CD11b/CD18-mediated neutrophil adhesion. NPC-18915 free base induces shedding of L-selectin on the neutrophil surface, thereby reducing endothelial cell adhesion. NPC-18915 free base inhibits calcium ionophore-induced LTB4 synthesis in neutrophils. NPC-18915 free base reduces the severity of TNBS-induced acute and recurrent colitis in rat experiments. NPC-18915 free base can be used in studies related to colitis.
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- CAS. Nr.: 179487-75-3
- Formel: C23H16O3
- Molecular Weight:340.37
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
LTB4 |
In Vitro
NPC-18915 (0.001-100 μg/mL; 10 min pre-incubation, 30 min post-stimulation) free base almost completely eliminates calcium ionophore-induced LTB4 synthesis in rat peritoneal neutrophils at concentrations of 10 μg/mL and 100 μg/mL, while no such effect is observed at lower concentrations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
NPC-18915 (10 mg/kg; i.p.; 1 hour before each subcutaneous injection of TNBS; for 3 consecutive days) free base reduces colon damage and granulocyte infiltration in male Wistar rats with recurrent TNBS-induced colitis, and restores all indicators to the levels of non-recurrent rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 200-225 g, acute colitis induced by intracolonic TNBS instillation)[1]
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Dosage:0.2 mg/kg (pre-induction); 2 mg/kg (pre-induction); 10 mg/kg (pre-induction); 10 mg/kg (post-induction)
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Administration:i.p.; every 12 h; 4 days (pre-induction); i.p.; every 12 h; 4 days (post-induction starting 48 h after induction)
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Result:Reduced colonic damage scores significantly at 2 mg/kg and 10 mg/kg pre-induction doses.
Reduced diarrhea incidence to 4 of 8 rats at 10 mg/kg pre-induction dose.
Reduced colon wall thickness to 1.76 mm at 2 mg/kg pre-induction dose.
Reduced colon wall thickness to 2.25 mm at 10 mg/kg pre-induction dose.
Did not significantly affect colonic myeloperoxidase activity at any pre-induction dose.
Did not significantly affect colonic damage scores, diarrhea incidence, adhesion formation, colon wall thickness, or myeloperoxidase activity at 10 mg/kg post-induction dose.
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Animal Model:Wistar (male, 200-225 g, reactivated colitis induced by subcutaneous TNBS 6 weeks after initial intracolonic TNBS-induced acute colitis)[1]
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Dosage:10 mg/kg
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Administration:i.p.; 1 h before each subcutaneous TNBS injection; over 3 days
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Result:Reduced colonic macroscopic damage scores significantly to levels not different from non-reactivated rats.
Reduced histological damage scores significantly to levels not different from non-reactivated rats.
Reduced myeloperoxidase activity significantly to levels not different from non-reactivated rats.
Chemical Information
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CAS. Nr. 179487-75-3
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Molecular Weight 340.37
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Formel C23H16O3
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SMILES
OC(C(C=C1)=CC=C1/C=C/C2=C(C=CC=C2)C3=CC4=CC=CC=C4O3)=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)
NPC-18915 free base Related Classifications
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