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
生物活性
製品説明
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) |
体外実験
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.
体内実験
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.
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 (290 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)