R59949

製品コードE0082 バッチE008201

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₈H₂₅F₂N₃OS

分子量

489.58

CAS No.

120166-69-0

Solubility (25°C)*

体外

DMSO

98 mg/mL (200.17 mM)

Ethanol

2 mg/mL (4.08 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (10.21mM)	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 Tween80 to the above system, mix evenly to make it clear; 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.

* <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	R59949, a diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM, inhibits inducible nitric oxide production through decreasing transplasmalemmal L-arginine uptake in vascular smooth muscle cells. R59949 strongly inhibits type I DGK a and γ, and moderately attenuates type II DGK θ and κ.
in vitro	R59949 is a pan diacylglycerol kinase (DGK) inhibitor, which inhibits inducible NO production through decreasing transplasmalemmal L-arginine uptake in rat aortic smooth muscle cells (RASMCs).^[1]
in vivo	R59949 upregulates the expression of PHD-2, also downregulates HIF-1α and vascular endothelial growth factor (VEGF) in the retina of oxygen-induced retinopathy (OIR) mice, suggesting a potential possibility that this compound suppresses retinal neovascular pathophysiology via PHD2/HIF-1α/VEGF pathway.^[2]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	rat aortic smooth muscle cells (RASMCs)
	濃度	10 µM
	反応時間	30 min
	実験の流れ	RASMCs are prepared from adult male Wistar rats and cultured in DMEM containing 10% FBS under 5% CO2 at 37 ℃. Cultured cells showing a confluent condition in a 24-well plate are used for experiments. The cells are pretreated with R59949 at 10 μM or cycloheximide at 1 μM at 30 min before stimulation with IL-1β at 10 ng/ml or a vehicle for 24 h. Measurement of NOX is performed in the presence of nitrate reductase using a commercial kit. After incubation with nitrate reductase at room temperature for 2 h, aliquots of the culture medium are mixed with Griess reagent (1% sulphanilamide/0.1% N-(1-naphthyl) ethylenediamine dihydrochloride in 5% phosphoric acid). The mixture is then incubated at room temperature for 10 min, and its absorbance is measured at 540 nm using a photometer.
動物実験	動物モデル	C57BL/6J mice
	投薬量	10 μg/g/day
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/27909743/
https://pubmed.ncbi.nlm.nih.gov/25451596/

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：

A light-controlled phospholipase C for imaging of lipid dynamics and controlling neural plasticity [ Cell Chem Biol, 2024, S2451-9456(24)00090-4]	PubMed: 38582083

A light-controlled phospholipase C for imaging of lipid dynamics and controlling neural plasticity [ Cell Chem Biol, 2024, S2451-9456(24)00090-4]

PubMed: 38582083

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。