ABT-080
Based on 1 Customer Validation
ABT-080 is an orally active inhibitor of leukotriene biosynthesis that targets 5-lipoxygenase-activating protein (FLAP). ABT-080 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 blocks the leukotriene pathway leading to the synthesis of LTB4 and LTC4, but does not block PGH2 biosynthesis. ABT-080 inhibits leukotriene biosynthesis and bronchoconstriction in mouse models. ABT-080 is used in research related to asthma, pleurisy and allergy.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.42%
- No. CAS: 189498-57-5
- Fòrmula: C37H31N2NaO4
- Peso molecular:590.64
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
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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) |
In Vitro
ABT-080 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 inhibits LTB4 production in human whole blood stimulated by calcium ionophore, with an IC50 of 13000 nM[1].
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 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.
In Vivo
ABT-080 (1.0-10 mg/kg; p.o.) 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].
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].
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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No. CAS 189498-57-5
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Appearance Solid
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Peso molecular 590.64
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Fòrmula C37H31N2NaO4
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Color Off-white to light yellow
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SMILES
O=C(CCC(C)(C1=CC=C(C=C1)OCC2=NC3=CC=CC=C3C=C2)C4=CC=C(C=C4)OCC5=NC6=CC=CC=C6C=C5)O[Na]
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Synonyms
VML-530
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ABT-080 Related Classifications
HY-113628 Related Classifications
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