GSK0660

製品コードS5817 バッチS581701

印刷

化学情報

Chemical Structure 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
* <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 is a potent PPARβ/δ antagonist with a pIC50 of 6.8 (binding assay IC50 = 155 nM; antagonist assay IC50 = 300 nM) and is nearly inactive on PPARα and PPARγ with IC50s above approximately 10 μM.
in vitro GSK0660 inhibits HRMEC (human retinal microvascular endothelial cells) proliferation and differentiation[2].
in vivo GSK0660 is rapidly cleared and does not accumulate in the blood in vivo[1]. GSK0660 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[2].

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.

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
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。

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