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.
For research use only. We do not sell to patients.
- CAS No.: 189498-56-4
- Formula: C37H32N2O4
- Molecular Weight:568.66
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
LTB4 20 nM (IC50, intact human neutrophils) |
LTB4 13 μM (IC50, human whole blood) |
LTC4 0.16 nM (IC50, mouse peritoneal macrophages) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| PMNL | IC50 |
23 nM
Compound: 17; ABT-080
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Inhibition of Leukotriene biosynthesis in calcium ionophore A-23187 stimulated human PMNL cells assessed as inhibition of LTB4 formation by enzyme immunoassay
Inhibition of Leukotriene biosynthesis in calcium ionophore A-23187 stimulated human PMNL cells assessed as inhibition of LTB4 formation by enzyme immunoassay
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[PMID: 28784429] |
In Vitro
ABT-080 free base inhibits LTB4 production in human whole blood stimulated by calcium ionophore, with an IC50 of 13000 nM[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.
Parmacokinetics
In Vivo
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].
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 No. 189498-56-4
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Molecular Weight 568.66
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ABT-080 free base Related Classifications
HY-113628A Related Classifications
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