貨號	規(guī)格	價(jià)格	上海	北京	武漢	南京
S81673-1mg	99.8%	￥216.00 S81673-1mg ￥216.00 現(xiàn)貨	5 5	-	-	-
S81673-2mg	99.8%	￥304.00 S81673-2mg ￥304.00 現(xiàn)貨	7 7	-	-	-
S81673-5mg	99.8%	￥520.00 S81673-5mg ￥520.00 現(xiàn)貨	6 6	-	-	-
S81673-10mg	99.8%	￥800.00 S81673-10mg ￥800.00 現(xiàn)貨	6 6	-	-	-
S81673-25mg	99.8%	￥1480.00 S81673-25mg ￥1480.00 現(xiàn)貨	5 5	-	-	-
S81673-50mg	≥99%	￥2880.00 S81673-50mg ￥2880.00 2-3天	0 貨期：2-3天	-	-	-
S81673-100mg	≥99%	￥5200.00 S81673-100mg ￥5200.00 2-3天	0 貨期：2-3天	-	-	-

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產(chǎn)品介紹

GSK0660是有效的PPARβ/δ拮抗劑，pIC50為6.8。在濃度高達(dá)近于10 μM時(shí)，對PPARα和PPARγ沒有活性

產(chǎn)品描述：

GSK0660是有效的PPARβ/δ拮抗劑，pIC50為6.8。在濃度高達(dá)近于10 μM時(shí)，對PPARα和PPARγ沒有活性

靶點(diǎn)：

PPAR-β/δ(binding assay):155 nM;PPAR

體外研究：

GSK0660 inhibits HRMEC (human retinal microvascular endothelial cells) proliferation and differentiation

體內(nèi)研究：

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

細(xì)胞實(shí)驗(yàn)：

Cell lines: HRMECs Concentrations: 0.01, 0.1, or 1.0 μM Incubation Time: 6 h Method: 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.

動物實(shí)驗(yàn)：

Animal Models: Sprague-Dawley rat Dosages: 0.2 or 1.0 mg/kg Administration: i.p.

參考文獻(xiàn)：

1. Shearer BG, et al. Identification and characterization of a selective peroxisome proliferator-activated receptor beta/delta (NR1C2) antagonist. Mol Endocrinol. 2008, 22(2):523-9. 2. Megan E. Capozzi, et al. Peroxisome Proliferator-Activated Receptor-β/δ Regulates Angiogenic Cell Behaviors and Oxygen-Induced Retinopathy. Invest Ophthalmol Vis Sci. 2013, 54(6): 4197–4207.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.39 ml	11.948 ml	23.896 ml
5 mM	0.478 ml	2.39 ml	4.779 ml
10 mM	0.239 ml	1.195 ml	2.39 ml
50 mM	0.048 ml	0.239 ml	0.478 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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