受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C15H11FN2 |
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分子量 | 238.26 | CAS No. | 163239-22-3 | |
Solubility (25°C)* | 体外 | DMSO | 48 mg/mL (201.46 mM) | |
Ethanol | 25 mg/mL (104.92 mM) | |||
Water | 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 | 680C91 is a potent and selective inhibitor of TDO with Ki of 51 nM. |
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in vitro | 68OC91 is a potent (Ki = 51 nM) and selective TDO inhibitor with no inhibitory activity against indoleamine 2,3-dioxygenase (EC 1.13.11.17), monoamine oxidase A and B, 5-HT uptake and 5-HT1A,1D,2A and 2c receptors at a concentration of 10 μM. 68OC91 has no effect on the binding of tryptophan to serum albumin in plasma and inhibited TDO competitively with respect to its substrate tryptophan. 68OC91 inhibits the catabolism of tryptophan by rat liver cells and rat liver perfused in situ.[1] |
in vivo | The catabolism of L-[ring-2-14C]-tryptophan and a load dose of tryptophan (100 mg/kg) in vivo are inhibited by prior administration of 68OC91. Administration of 68OC91 alone produces marked increases in brain tryptophan, 5-HT and 5-HIAA. A load dose of tryptophan (100 mg/kg), producing increases in brain tryptophan 4-fold greater than that seen with 68OC91, does not increase brain 5-HT and 5-HIAA to levels greater than those seen with 68OC91 and produces a shorter-lasting increase in these parameters.[1] |
細胞アッセイ | 細胞株 | rat liver cells |
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濃度 | 0.1 μM, 0.5 μM, 2 μM | |
反応時間 | 0 min - 120 min | |
実験の流れ | The combined concentration of the L-[ring-2-14C]-tryptophan and non-labelled L-tryptophan used in the assays is 20 μM and is added either with or without 68OC91 at time zero. |
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動物実験 | 動物モデル | Male Wistar rats |
投薬量 | 15 mg/kg | |
投与方法 | Oral gavage |
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Targeting Tryptophan Catabolism in Ovarian Cancer to Attenuate Macrophage Infiltration and PD-L1 Expression [ Cancer Res Commun, 2024, 4(3):822-833] | PubMed: 38451784 |
Serotonin reduction in post-acute sequelae of viral infection [ Cell, 2023, 186(22):4851-4867.e20] | PubMed: 37848036 |
Identification and Characterization of a Novel Dual Inhibitor of Indoleamine 2,3-dioxygenase 1 and Tryptophan 2,3-dioxygenase [ Int J Tryptophan Res, 2022, 15:11786469221138456] | PubMed: 36467776 |
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。