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Art. -Nr.: HY-113628

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ABT-080

Name: ABT-080
Brand: MedChemExpress
SKU: HY-113628
Price: 79.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: VML-530)

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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.

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Reinheit : 98.42%
CAS. Nr.: 189498-57-5
Formel: C₃₇H₃₁N₂NaO₄
Molecular Weight:590.64

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

ABT-080 Chemical Structure

CAS. Nr.: 189498-57-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

LTB4

20 nM (IC₅₀, intact human neutrophils)

LTB4

13 μM (IC₅₀, human whole blood)

LTC4

0.16 nM (IC₅₀, mouse peritoneal macrophages)

In Vitro

Lipid Inflammatory MediatorsInnate Immunity

Lipid Inflammatory Mediators

Innate Immunity

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].

Innate Immunity

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.

In Vivo

InflammasomeOthersInnate Immunity

Inflammasome

The free base of ABT-080 (3.0 mg/kg; p.o.) inhibits leukotriene biosynthesis in a rat pleurisy model, with an ED₅₀ of 3.0 mg/kg^[1].

Others

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].

Innate Immunity

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.

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)
Administration:

p.o.; single dose (1 hour pre-challenge)
Result:

Inhibited leukotriene biosynthesis with an ED₅₀ of 3.0 mg/kg.

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]
Dosage:

2.5 mg/kg (LTB4 ED₅₀); 1.0 mg/kg (LTE4 ED₅₀); 10 mg/kg (duration-of-action)
Administration:

p.o.; single dose
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.

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)
Administration:

p.o.; twice daily; 4 days
Result:

Inhibited leukotriene formation with an ED₅₀ of 3.3 mg/kg.
Inhibited eosinophil influx with an ED₅₀ of 3.5 mg/kg.

Animal Model:

Guinea pigs^[1]
Dosage:

0.4 mg/kg (ED₅₀)
Administration:

p.o.
Result:

Inhibited antigen-induced bronchoconstriction with an ED₅₀ of 0.4 mg/kg.

Chemical Information

CAS. Nr. 189498-57-5
Appearance Solid
Molecular Weight 590.64
Formel C₃₇H₃₁N₂NaO₄
Color Off-white to light yellow
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]
Synonyms

VML-530
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Kolasa T, et al. Symmetrical bis(heteroarylmethoxyphenyl)alkylcarboxylic acids as inhibitors of leukotriene biosynthesis. Journal of medicinal chemistry. 2000 Aug 24;43(17):3322-34. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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ABT-080