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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C25H35N3O2 |
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分子量 | 409.56 | CAS No. | 947303-87-9 | |
Solubility (25°C)* | 体外 | DMSO | 82 mg/mL (200.21 mM) | |
Water | 82 mg/mL (200.21 mM) | |||
Ethanol | 82 mg/mL (200.21 mM) | |||
* <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 | PF 429242 is known as a S1P inhibitor with an IC50 of 170 nM, showing no significant inhibition of trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, or furin at concentrations up to 100 μM and only modest inhibition of urokinase (IC50 = 50 μM) and factor Xa (IC50 = 100 μM). |
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in vitro | In cultured human liver (Hep-G2) cells, PF-429242 prevents proteolytic processing and nuclear translocation of SREBP, reduces the expression of key genes involved in cholesterol synthesis and fatty acid synthesis, and inhibits both pathways in the absence of any cytotoxicity[1]. The addition of PF-429242 suppresses the viral propagation of all serotypes of DENV in several primate-derived cells[2]. |
in vivo | PK data for PF-429242 show that it had rapid clearance (CL = 75 ml/min/kg) and poor oral bioavailability (5%) in rats[1]. |
細胞アッセイ | 細胞株 | HeLa cells |
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濃度 | 3 to 300 µM | |
反応時間 | 72 h | |
実験の流れ | HeLa cells are seeded in MEM supplemented with 2% FCS and 0.2 mM nonessential amino acids, which contained 3 to 300 µM of PF-429242. After 72 h post drug treatment, a CellTiter-Glo mixture is added to the cultured cells, and the intracellular ATP is measured for luminescence intensity with ARVO MX/Light 1420 Multilabel/Luminescence counter. |
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動物実験 | 動物モデル | CD-1 mice |
投薬量 | 10 and 30 mg/kg/dose | |
投与方法 | i.p. |
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The Scap-SREBP1-S1P/S2P lipogenesis signal orchestrates the homeostasis and spatiotemporal activation of NF-κB [ Cell Rep, 2023, 42(6):112586] | PubMed: 37267109 |
RORγ Is a Targetable Master Regulator of Cholesterol Biosynthesis in a Cancer Subtype [ Nat Commun, 2019, 11;10(1):4621] | PubMed: 31604910 |
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。