AM-643
AM-643 is a FLAP inhibitor with human IC50 of 2 nM, oral activity, and dermal activity.AM-643 selectively inhibits FLAP, reduces leukotriene biosynthesis and reduces inflammatory ear swelling.AM-643 can be used for the research of skin disorders involving leukotriene production.
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- CAS. Nr.: 1233114-22-1
- Formel: C36H40N4O4S
- Molecular Weight:624.80
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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
Beschreibung
In Vitro
AM-643 (compound 6) potently inhibits 3H-ligand binding to human polymorphonuclear leukocyte-derived FLAP membranes with an IC50 of 2 nM[1].
AM-643 potently inhibits calcium ionophore-induced LTB4 synthesis in isolated human leukocytes with an IC50 of 0.6 nM[1].
AM-643 (15 min-5 h) inhibits calcium ionophore-induced LTB4 synthesis in human whole blood with an IC50 of 161 nM after 15 minutes of pre-incubation and an IC50 of 81 nM after 5 hours of pre-incubation[1].
AM-643 inhibits human CYP 3A4 with an IC50 of 8.8 μM, human CYP 2C9 with an IC50 of 4.5 μM, and does not inhibit human CYP 2D6 at concentrations up to 30 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AM-643 (0.01, 0.1%; topical; single dose) produces a 61% inhibition of arachidonic acid-induced ear edema, a 37% reduction in CysLT concentrations, and a 55% reduction in LTB4 concentrations in mouse ear tissue in vivo in a concentration-dependent manner[1].
AM-643 (10 mg/mL; topical; single dose; occluded for 24 hours) causes no dermal irritancy and results in detectable systemic exposure in abraded healthy male rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1233114-22-1
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Molecular Weight 624.80
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Formel C36H40N4O4S
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SMILES
O=C(O)C(C)(C)CC1=C(SC(C)(C)C)C=2C=C(OCC3=NC=C(C=C3)C)C=CC2N1CC=4C=CC(=CC4)C5=NC=C(OC)C=N5
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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)
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