GSK0660

製品コードS5817 バッチS581701

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₉H₁₈N₂O₅S₂

分子量

418.49

CAS No.

1014691-61-2

Solubility (25°C)*

体外

DMSO

84 mg/mL (200.72 mM)

Water

Insoluble

Ethanol

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。	4.200mg/ml (10.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 84 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 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。	0.600mg/ml (1.43mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 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	GSK0660は、pIC50が6.8（結合アッセイIC50 = 155 nM；拮抗アッセイIC50 = 300 nM）の強力なPPARβ/δアンタゴニストであり、PPARαおよびPPARγに対してはIC50が約10 μMを超え、ほとんど不活性です。
in vitro	GSK0660 inhibits HRMEC (human retinal microvascular endothelial cells) proliferation and differentiation.
in vivo	GSK0660 is rapidly cleared and does not accumulate in the blood in vivo. This compound is efficacious against retinal NV when administered by IVIT or IP injection. Intravitreal injection has the advantages of producing high levels of drug at active sites of neovascular disease, but deleterious side effects are associated with this route of drug administration, including endophthalmitis, cataractogenesis, and glaucoma. Systemic administration could avoid these side effects, but it is hampered by the need for repeated dosing to obtain target concentrations of active drug in diseased tissues. It also needlessly exposes disease-free organs and tissues to active drug.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HRMECs
	濃度	0.01, 0.1, or 1.0 μM
	反応時間	6 h
	実験の流れ	HRMECs were seeded in six-well plates at 2 × 10⁵ cells/well and maintained under standard tissue culture conditions. At 80% confluency, the cells were serum starved for 12 hours, then treated on a background of 0.5% serum-containing vehicle (0.1% DMSO) or PPAR-β/δ agonist GW0742 (0.01, 0.1, or 1.0 μM) or on a background of 2% serum-containing vehicle or PPAR-β/δ antagonist GSK0660 (0.01, 0.1, or 1.0 μM) for 6 hours. Cells were washed twice with cold PBS and total RNA was collected. Total RNA isolated from the culture wells was reverse transcribed. Quantitative RT-PCR was performed.
動物実験	動物モデル	Sprague-Dawley rat
	投薬量	0.2 or 1.0 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/17975020/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3687964/

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：

Blastocyst-Derived Lactic Acid May Regulate S100A6 Expression and Function in Mouse Decidualization via Stimulation of Uterine Epithelial Arachidonic [ Cells, 2024, 13(3):206.]	PubMed: 38334598
Blastocyst-Derived Lactic Acid May Regulate S100A6 Expression and Function in Mouse Decidualization via Stimulation of Uterine Epithelial Arachidonic Acid Secretion [ Cells, 2024, 13(3)206]	PubMed: 38334598
Embryo-derive TNF promotes decidualization via fibroblast activation [ Elife, 2023, 12e82970]	PubMed: 37458359
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。