PF 429242

製品コードS6418 バッチS641803

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₅H₃₅N₃O₂

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)

体内（毎回新しく調製した物を用意してください）

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.1mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 82 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.51mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 10.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

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).
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].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HeLa cells
	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.
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.

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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。