Vidofludimus

製品コードS7262 バッチS726201

印刷

化学情報

Synonyms

SC12267, 4SC-101

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₀H₁₈FNO₄

分子量

355.36

CAS No.

717824-30-1

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

100 mg/mL (281.4 mM)

Ethanol (warmed with 50ºC water bath)

1 mg/mL (2.81 mM)

Water

Insoluble

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

5.0mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween-80 to the above system, mix evenly to clarify it; then Continue to add 500 μL ddH2O to adjust the volume to 1 mL. 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	Vidofludimus (SC12267, 4SC-101) is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH. Vidofludimus calcium (IMU-838) is investigated as a potential treatment option for COVID-19. Phase 2.
in vitro	Vidofludimus causes a concentration dependent inhibition of phytohemagglutinin-stimulated PBMC proliferation via the inhibition of pyrimidine de novo synthesis. ^[1] Vidofludimus attenuates IL-17 secretion from colonic strips by inhibition of STAT3 and NF-κB activation. ^[2]
in vivo	In MRL^lpr/lpr mice, Vidofludimus (300 mg/kg, p.o.) reduces systemic autoimmunity and improves Lupus Nephritis. ^[1] In Rats, Vidofludimus (60 mg/kg, p.o.) effectively reduces macroscopic and histological pathology and the numbers of CD3+ T cells. ^[2] In a rat model of renal transplantation, Vidofludimus (20 mg/kg, p.o.) prolongs survival, paralleled by amelioration of histologic signs of acute rejection. ^[3]

プロトコル(参考用のみ)

キナーゼアッセイ	DHODH inhibition assay
キナーゼアッセイ	In vitro DHODH inhibition assay mixture contains 50 μM decycloubiquinone, 100 μM dihydroorotate, and 60 μM 2,6-dichloroindophenol. The amount of enzyme is adjusted such that an average slope of approximately 0.2 AU/min will be achieved in the assay for the positive control (eg, without inhibitor). Measurements are conducted in 50 mM TrisHCl, 150 mM KCl, 0.1% Triton X-100, and pH 8.0 at 30°C in a final volume of 1 ml. The components are mixed, and the reaction is started by adding dihydroorotate. The reaction is followed spectrophotometrically by measuring the decrease in absorption at 600 nm for 2 minutes. The assay is linear in time and enzyme concentration. Inhibitory studies are conducted in a standard assay with additional variable amounts of inhibitor. For the determination of the IC50 values (concentration of inhibitor required for 50% inhibition), eight different inhibitor concentrations are applied. Each data point is recorded in triplicates on a single measurement day.
細胞アッセイ	細胞株	PBMCs
	濃度
	反応時間	48 h
	実験の流れ	Human PBMCs from healthy human donors are purified by centrifugation over Ficoll-Hypaque. Purified PBMCs are then washed twice with phosphate-buffered saline and resuspended in RPMI1640 culture medium supplemented with 10% heat inactivated fetal calf serum, 1.5 mM l-glutamine, 100 U penicillin/ml, and 100 mg streptomycin/ml, and treated with compounds at the indicated concentrations for 48 hours. The vehicle for 4SC-101 is DMSO. After incubation, proliferation is assessed by using the cell proliferation colorimetric BrdU-enzyme-linked immunosorbent assay kit according to the manufacturer’s instructions.
動物実験	動物モデル	MRL^lpr/lpr mice
	投薬量	300 mg/kg/day
	投与方法	p.o.

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：

Hydrogel-Based Pre-Clinical Evaluation of Repurposed FDA-Approved Drugs for AML [ Int J Mol Sci, 2023, 24(4)4235]	PubMed: 36835644
Identification of clinical candidates against West Nile Virus by activity screening in vitro and effect evaluation in vivo [ J Med Virol, 2022, 10.1002/jmv.27891]	PubMed: 35644833
Cerpegin-derived furo[3,4-c]pyridine-3,4(1H,5H)-diones enhance cellular response to interferons by de novo pyrimidine biosynthesis inhibition. [ Eur J Med Chem, 2019, 10.1016/j.ejmech.2019.111855]	PubMed: 31740051

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。