ZM 230487
ZM 230487 (ICI-230487) is an orally active, selective, non-redox 5-lipoxygenase (5-LO) inhibitor. ZM 230487 potently inhibits antigen-induced LTD4 release (IC50 ≈ 0.2 µM), but does not affect the release of TXB2 and histamine. ZM 230487 specifically blocks eosinophil accumulation and partial bronchoconstriction in guinea pig models. ZM 230487 can be used in studies related to allergic inflammation.
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- CAS. Nr.: 155944-23-3
- Formel: C24H26FNO4
- Molecular Weight:411.47
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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
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Biologische Aktivität
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5-LO |
LTD4 |
ZM 230487 (0.03-1.0 μM) potently inhibits antigen-induced leukotriene D4 release from sensitized guinea pig lung parenchymal fragments prepared in vitro, with an IC50 of 0.2 μM, but exerts no significant effect on antigen-induced thromboxane B2 or histamine release[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ZM 230487 (10 nmol per site; intradermal injection; single administration) significantly inhibits eosinophil accumulation (with an inhibition rate of 44%-72%), but exerts no effect on edema formation in the guinea pig passive cutaneous anaphylaxis model[1].
ZM 230487 (1 mg/kg; intravenous injection; single administration) potently inhibits antigen-induced bronchoconstriction in passively sensitized guinea pigs with an inhibition rate of 90%, and exerts no non-specific effect on methacholine-induced pulmonary responses[2].
ZM 230487 (0.4 mg/kg; p.o.; single administration) potently inhibits leukotriene B4 synthesis in a zymosan-induced inflammatory rat air pouch model, with an oral ED50 of 0.4 mg/kg at 3 h post-administration[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Harlan Porcellus (male, 350-400 g)[1]
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Dosage:1, 10, 100 pmol; 1, 10, 100 nmol per site
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Administration:i.d.; single dose
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Result:Abolished AA-induced 111In-eosinophil accumulation with an IC50 of approximately 2 pmol per site.
Reduced AA-induced 111In-eosinophil accumulation from 11880 to 273 cells per skin site at 10 nmol per site.
Slightly enhanced small AA-induced oedema response at lower doses.
Inhibited AA-induced oedema response by up to 40% at doses greater than 1 pmol per site.
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Animal Model:Harlan Porcellus (male, 350-400 g)[1]
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Dosage:10 nmol per site
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Administration:i.d.; single dose
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Result:Inhibited PCA-induced 111In-eosinophil accumulation by 72% at the 0.1 μg per site BGG dose.
Inhibited PCA-induced 111In-eosinophil accumulation by 44% at the 1.0 μg per site BGG dose.
Had no effect on PCA-induced oedema formation.
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Animal Model:albino (male, 250-400 g, passively sensitized to ovalbumin via i.p. injection of donor serum from actively sensitized guinea pigs 42 h prior to experiment)[2]
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Dosage:1 mg/kg
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Administration:i.v.; single dose
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Result:Inhibited peak antigen-induced increases in pulmonary resistance by 90%.
Did not alter methacholine-induced changes in pulmonary conductance, with a mean -log ED50 of 8.16.
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Animal Model:albino (male)[2]
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Dosage:0.4 mg/kg
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Administration:p.o.; single dose
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Result:Exhibited an ED50 value of 0.4 mg/kg at 3 h for inhibition of leukotriene B4 synthesis.
Chemical Information
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CAS. Nr. 155944-23-3
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Molecular Weight 411.47
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Formel C24H26FNO4
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SMILES
O=C1N(C2=C(C=C1)C=C(C=C2)COC3=CC(C4(CCOCC4)OC)=CC(F)=C3)CC
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Synonyms
ICI-230487
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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]. Teixeira MM, et al. Effect of a 5-lipoxygenase inhibitor, ZM 230487, on cutaneous allergic inflammation in the guinea-pig. British journal of pharmacology. 1994 Apr;111(4):1205-11. [Content Brief]
[2]. Kusner EJ, et al. The 5-lipoxygenase inhibitors ZD2138 and ZM230487 are potent and selective inhibitors of several antigen-induced guinea-pig pulmonary responses. European journal of pharmacology. 1994 May 23;257(3):285-92. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
ZM 230487 Related Classifications
HY-120095 Related Classifications
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- ZM 230487
- 155944-23-3
- ICI-230487
- ZM230487
- ZM-230487
- ICI230487
- ICI 230487
- Lipoxygenase
- Leukotriene Receptor
- peptidoleukotrienes
- leukotriene D4
- cutaneous allergic inflammation
- leukotriene synthesis
- LTB4
- guinea-pig lung parenchyma segments
- 5-lipoxygenase
- arachidonic acid
- eosinophil accumulation
- PAF
- Inhibitor
- inhibitor
- inhibit