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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C25H27N5 |
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分子量 | 397.52 | CAS No. | 162640-98-4 | |
Solubility (25°C)* | 体外 | DMSO | 80 mg/mL (201.24 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | AT-56 is an orally active and selective inhibitor of lipocalin-type prostaglandin (PG) D synthase (L-PGDS) with Ki of 75 μM and IC50 of 95 μM. |
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in vitro | AT-56 inhibits human and mouse L-PGDSs in a concentration (3–250 μm)-dependent manner. AT-56 inhibits the L-PGDS activity in a competitive manner against the substrate PGH2 (Km = 14 μm) with a Ki value of 75 μm. AT-56 inhibits the production of PGD2 by L-PGDS-expressing human TE-671 cells after stimulation with Ca2+ ionophore (5 μm A23187) with an IC50 value of about 3 μm without affecting their production of PGE2 and PGF2α.[1] |
in vivo | Orally administered AT-56 (<30 mg/kg body weight) decreases the PGD2 production to 40% in the brain of H-PGDS-deficient mice after a stab wound injury in a dose-dependent manner without affecting the production of PGE2 and PGF2α and also suppresses the accumulation of eosinophils and monocytes in the bronco-alveolar lavage fluid from the antigen-induced lung inflammation model of human L-PGDS-transgenic mice.[1] |
細胞アッセイ | 細胞株 | TE-671 cells, MEG-01S cells |
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濃度 | 0 - 100 μM | |
反応時間 | 10 min | |
実験の流れ | TE-671 (1×106 cells/well) and MEG-01S (5×105 cells/well) are seeded into multiplates and cultured in Dulbecco's modified Eagle's medium supplemented with 10% heat-inactivated fetal bovine serum, 4 mM L-glutamine, 4.5 g/liter glucose, 100 units/ml penicillin, and 100 μg/ml streptomycin sulfate under a 5% CO2 atmosphere at 37 ℃. MEG-01S cells are caused to differentiate by treatment with 12-O-tetradecanoylphorbol-13-acetate to express H-PGDS and COX-1. After the cells have been cultured for 1 day, AT-56 is added to them at different doses ranging from 0 to 100 μM, and the cells are then incubated at 37 ℃ for 10 min. Thereafter, they are stimulated with a calcium ionophore, A23187 (5 μM), at 37 ℃ for 15 min. The culture media were harvested and centrifuged at 10,000 × g for 5 min to remove the cells, and the supernatant is removed and stored at 80 ℃ until the measurements of PGs can be made. |
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動物実験 | 動物モデル | H-PGDS KO mice (14–16-week-old males or females weighing 25–30 g, C57BL/6 strain) |
投薬量 | 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg | |
投与方法 | Oral gavage |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。