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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.42%
- CAS 番号: 189498-57-5
- 分子式: C37H31N2NaO4
- 分子量:590.64
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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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 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.
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.
化学情報
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CAS 番号 189498-57-5
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性状 Solid
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分子量 590.64
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分子式 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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別名
VML-530
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
ABT-080 関連分類
HY-113628 関連分類
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