ABT-080 free base
ABT-080 free base is an orally active inhibitor of leukotriene biosynthesis that targets 5-lipoxygenase-activating protein (FLAP). ABT-080 free base inhibits leukotriene production in intact human neutrophils, mouse peritoneal macrophages and human whole blood, with IC50 values of 20 nM, 0.16 nM and 13 μM, respectively. ABT-080 free base blocks the leukotriene pathway leading to the synthesis of LTB4 and LTC4, but does not block PGH2 biosynthesis. ABT-080 free base inhibits leukotriene biosynthesis and bronchoconstriction in mouse models. ABT-080 is used in research related to asthma, pleurisy and allergy.
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- CAS. Nr.: 189498-56-4
- Formel: C37H32N2O4
- Molecular Weight:568.66
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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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LTB4 20 nM (IC50, intact human neutrophils) |
LTB4 13 μM (IC50, human whole blood) |
LTC4 0.16 nM (IC50, mouse peritoneal macrophages) |
ABT-080 free base potently inhibits the production of LTB4 in intact human neutrophils stimulated by calcium ionophores, with an IC50 of 20 nM. This inhibitory effect shows weak reversibility, and binding to serum albumin significantly reduces its inhibitory activity[1].
ABT-080 free base inhibits LTB4 production in human whole blood stimulated by calcium ionophore, with an IC50 of 13000 nM[1].
The free base form of ABT-080 (300 μM) does not inhibit the 5-lipoxygenase-catalyzed oxidation of arachidonic acid in the supernatant of sonicated RBL-2H3 cells[1].
ABT-080 free base exhibits inhibitory activity against LTC4 production in zymosan-stimulated mouse peritoneal macrophages (IC50 = 0.16 nM), with a 9000-fold higher selectivity for LTC4 over PGE2 (PGE2 IC50 = 1500 nM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ABT-080 (1.0-10 mg/kg; p.o.) free base inhibits the production of LTB4 (ED50 = 2.5 mg/kg) and LTE4 (ED50 = 1.0 mg/kg) in a rat peritoneal passive anaphylaxis model, and the 70% inhibitory effect on LTE4 persists for 8 h at a dose of 10 mg/kg[1].
The free base of ABT-080 (0.4 mg/kg; p.o.) inhibits antigen-induced bronchoconstriction in actively sensitized guinea pigs, with an ED50 of 0.4 mg/kg[1].
The free base form of ABT-080 (3.3-3.5 mg/kg; p.o.; twice daily; for 4 consecutive days) inhibits leukotriene production (ED50 = 3.3 mg/kg) and eosinophil infiltration (ED50 = 3.5 mg/kg) in a Brown Norway rat model of pulmonary inflammation, with an administration regimen of twice daily oral dosing for 4 consecutive days[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats were dosed with
experimental compounds in 0.2% HPMC 1 h before the
intrapleural injection of the calcium ionophore A-23187. The
rats were lightly anesthetized with penthrane and injected
intrapleurally with 0.5 mL of 2% ethanol in injectable saline
containing 20 μg of A-23187 (HY-N6687).[1] -
Dosage:3.0 mg/kg (ED50)
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Administration:p.o.; single dose (1 hour pre-challenge)
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Result:Inhibited leukotriene biosynthesis with an ED50 of 3.0 mg/kg.
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Animal Model:At Peritoneal Anaphylaxis Model. Rats were pas-sively sensitized to bovine serum albumin, and 3 h later theywere challenged in the peritoneal cavity with antigen[1]
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Dosage:2.5 mg/kg (LTB4 ED50); 1.0 mg/kg (LTE4 ED50); 10 mg/kg (duration-of-action)
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Administration:p.o.; single dose
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Result:Inhibited LTB4 production with an ED50 of 2.5 mg/kg.
Inhibited LTE4 production with an ED50 of 1.0 mg/kg.
Inhibited LTE4 production by 70% for up to 8 hours at a single oral dose of 10 mg/kg.
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Animal Model:Brown Norway rats wereBis(heteroarylmethoxyphenyl)alkylcarboxylic Acids Journal of Medicinal Chemistry, 2000, Vol. 43, No. 17 3333
orally dosed with inhibitors in 0.2% methylcellulose and theninjected in the central tail vein with Sephadex G-200. For thenext 3 days, the rats were dosed either once or twice a daywith either inhibitor or the vehicle control, 0.2% methylcel-lulose.[1] -
Dosage:3.3 mg/kg (leukotriene formation ED50); 3.5 mg/kg (eosinophil influx ED50)
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Administration:p.o.; twice daily; 4 days
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Result:Inhibited leukotriene formation with an ED50 of 3.3 mg/kg.
Inhibited eosinophil influx with an ED50 of 3.5 mg/kg.
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Animal Model:Guinea pigs[1]
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Dosage:0.4 mg/kg (ED50)
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Administration:p.o.
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Result:Inhibited antigen-induced bronchoconstriction with an ED50 of 0.4 mg/kg.
Chemical Information
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CAS. Nr. 189498-56-4
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Molecular Weight 568.66
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Formel C37H32N2O4
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SMILES
O=C(CCC(C1=CC=C(C=C1)OCC2=NC3=C(C=C2)C=CC=C3)(C)C4=CC=C(C=C4)OCC5=NC6=C(C=C5)C=CC=C6)O
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Synonyms
VML-530 free base
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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)
ABT-080 free base Related Classifications
HY-113628A Related Classifications
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