SM-15178
SM-15178 is a potent, orally active and selective leukotriene B4 (LTB4) receptor antagonist with an IC50 of 0.30 μM. SM-15178 attenuates LTB4 (HY-107608)-induced neutrophil accumulation in mouse skin and bronchoconstriction in guinea pigs. SM-15178 emonstrates significant anti-inflammatory efficacy across multiple animal models of inflammation. SM-15178 can be used for the research of chronic inflammatory diseases such as inflammatory bowel disease, psoriasis, and asthma.
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- CAS. Nr.: 146461-98-5
- Formel: C22H26N2O6
- Molecular Weight:414.46
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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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LTB4 0.30 μM (IC50) |
SM-15178 (30 min) inhibits LTB4 binding to human neutrophils in a dose-dependent manner (IC50 = 0.30 μM)[3].
SM-15178 (up to 30 μM; 15-90 min) inhibits LTB4-induced chemotaxis of mouse and rat neutrophils and guinea pig eosinophils (IC50 = 0.52-0.72 μM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
SM-15178 (5 mg/kg; i.v.; 2-30 min pre-LTB4, or 40 mg/kg; p.o.; 60 min pre-LTB4) potently inhibits LTB4-induced bronchoconstriction in guinea pigs[2].
SM-15178 (20-40 mg/kg; p.o.; single dose) suppresses LTB4-induced transient leukopenia in guinea pigs[3].
SM-15178 (5-100 mg/kg; p.o.; single dose) suppresses Arachidonic Acid-induced neutrophil infiltration in mice[3].
SM-15178 (10-100 mg/kg; p.o.; one day or 1 h before SRBC challenge) inhibits sheep red blood cells (SRBC)-induced paw edema in mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6N mice induced by LTB4[1]
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Dosage:5 mg/kg
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Administration:i.v.; single dose
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Result:Significantly reduced LTB4-induced neutrophil accumulation by 70.3%.
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Animal Model:Guinea pigs challenged with LTB₄[2]
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Dosage:5 mg/kg (i.v.); 40 mg/kg (p.o.)
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Administration:i.v.; 2, 10, or 30 min pre-LTB₄; p.o.; 60 min pre-LTB₄
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Result:Showed potent inhibitory activity against LTB₄-induced bronchoconstriction at all dosages.
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Animal Model:Male Hartley Guinea pigs (400-450 g) intravenously injected with LTB₄[3]
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Dosage:20, 40 mg/kg
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Administration:p.o.; single dose; 1 h pre-LTB4
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Result:Significantly suppressed LTB₄-induced transient leukopenia and LTB₄-induced bronchoconstriction.
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Animal Model:Male BALB/c (20-30 g) topically applied with Arachidonic Acid[3]
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Dosage:5, 25, 50, 100 mg/kg
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Administration:p.o.; single dose
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Result:Suppressed arachidonic acid-induced increases in myeloperoxidase (MPO) levels in a dose-dependent manner.
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Animal Model:Male BALB/c (25-30 g) injected with SRBC[3]
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Dosage:10, 25, 50, 100 mg/kg
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Administration:p.o.; one day or 1 hour before SRBC
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Result:Inhibited Arthus reaction-induced paw edema in a dose-dependent manner with a minimum effective dose of 25 mg/kg.
Chemical Information
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CAS. Nr. 146461-98-5
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Molecular Weight 414.46
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Formel C22H26N2O6
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SMILES
O=C(O)CCN(C(=O)C=1N=C(C=CC1)COC2=CC(O)=C(C=C2CC)C(=O)C)CC
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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
[1]. Ohnishi M, et al. Role of P-selectin in the migration of neutrophils to chemoattractant-induced cutaneous inflammation in mice. Inflammation. 2000;24(6):583-593. [Content Brief]
[3]. Ohmi N, et al. Pharmacological profile of a novel, orally active leukotriene B4 antagonist, SM-15178. Inflammation. 1994;18(2):129-140. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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