keep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Diquafosol tetrasodium (INS365) 是一种 P2Y2 受体激动剂,可刺激眼组织粘蛋白的分泌。它可改善泪膜稳定性和视觉功能,作为干眼症的局部治疗。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 256 | 现货 | ||
2 mg | ¥ 365 | 现货 | ||
5 mg | ¥ 592 | 现货 | ||
10 mg | ¥ 957 | 现货 | ||
25 mg | ¥ 1,750 | 现货 | ||
50 mg | ¥ 2,930 | 现货 | ||
100 mg | ¥ 4,330 | 现货 | ||
500 mg | ¥ 9,370 | 现货 |
产品描述 | Diquafosol Tetrasodium is a P2Y2 receptor agonist that stimulates the secretion of mucins from ocular tissues Diquafosol tetrasodium (INS365) improves tear film stability and visual function, as a topical treatment of dry eye disease. |
体外活性 | duration of exposure and diquafosol concentration significantly reduced cell survival and increased cell lysis.?On the other hand, no significant difference was observed in HA groups regardless of exposure time.?Cell viability significantly decreased after treatment for 1 hour with 30% diluted diquafosol and after treatment for 6 hours with all diluted diquafosol.?After treatment with all diluted diquafosol for 24 hours, cell viability decreased and lysis increased, and significant cellular damage was observed[1]. |
体内活性 | In a rat dry eye model, the P2Y(2) agonist INS365 was found to improve surface health, based on increases in tear fluid secretion, corneal epithelial resistance, and release of glycoprotein-containing moieties from goblet cells.??INS365 is a potential therapeutic agent for use in the treatment of dry eye syndrome[2]. |
细胞实验 | The viabilities of human corneal epithelial cells (HCECs) were determined using a MTT assay.?Cells (100 μl;?5×104 cell/mL) were plated in 96-well tissue-culture plates and incubated at 37℃ in 5% CO2 for 24 to 48 h until cultures were subconfluent.?Diquafosol (100 μl diluted 10%, 20%, or 30%) or 0.3% or 0.18% HA were added and incubated for 1, 6, or 24 h. DMEM (100 μl) was added to controls.?After 1, 6, and 24 h, plates were washed three times with PBS to remove the drugs.?Cell viabilities were evaluated after incubating for 24 h. MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide;?thiazoyl blue (5 mg/mL) was then added to each well.?Samples were incubated in the dark for 4 h at 37℃, and media were then removed.?Precipitates were resuspended indimethyl sulfoxide (100 μl;?DMSO, Sigma-Aldrich).?Absorbances were measured on a plate reader at 570 nm.?The experiment was performed in triplicate[1]. |
动物实验 | An SD rat dry eye model was used in which exorbital lacrimal gland extirpation decreased the Schirmer test score by at least 50%. After 8 weeks, when significant increases occurred in corneal epithelial permeability, Diquafosol tetrasodium(INS365)-containing eye drops were applied six times daily for the next 4 weeks at concentrations from 0.03% to 3.0%. Corneal barrier function was evaluated based on measurements with a modified anterior fluorometer of fluorescein penetrance at 1, 2, and 4 weeks after initial application. After INS365 application, the periodic acid-Schiff reagent (PAS)-stained area was evaluated in histologic sections of the tarsal and bulbar conjunctiva[2]. |
别名 | 地夸磷索四钠, INS365 |
分子量 | 878.23 |
分子式 | C18H22N4Na4O23P4 |
CAS No. | 211427-08-6 |
keep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 10 mM
DMSO: Insoluble
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O | 1 mM | 1.1387 mL | 5.6933 mL | 11.3865 mL | 28.4663 mL |
5 mM | 0.2277 mL | 1.1387 mL | 2.2773 mL | 5.6933 mL | |
10 mM | 0.1139 mL | 0.5693 mL | 1.1387 mL | 2.8466 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Diquafosol tetrasodium 211427-08-6 GPCR/G Protein Neuroscience P2Y Receptor Inhibitor inhibit INS 365 地夸磷索四钠 Diquafosol INS-365 INS365 inhibitor