| CAS |
No.211427-08-6 |
| 英文名称 |
Diquafosol tetrasodium |
| 别名 |
地夸磷索四钠 |
| 分子式 |
C18H22N4Na4O23P4 |
| 分子量 |
878.23 |
| 溶解性 |
Soluble in DMSO ≥10mg/mL(Need ultrasonic) |
| 纯度 |
≥98% |
| 外观(性状) |
White to off-white Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL |
MFCD18071356 |
| SMILES |
C1=CN(C(=O)NC1=O)C2C(C(C(O2)COP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OCC3C(C(C(O3)N4C=CC(=O)NC4=O)O)O)O)O.[Na+].[Na+].[Na+].[Na+] |
| InChIKey |
OWTGMPPCCUSXIP-FNXFGIETSA-J |
| InChI |
InChI=1S/C18H26N4O23P4.4Na/c23-9-1-3-21(17(29)19-9)15-13(27)11(25)7(41-15)5-39-46(31，32)43-48(35，36)45-49(37，38)44-47(33，34)40-6-8-12(26)14(28)16(42-8)22-4-2-10(24)20-18(22)30;;;;/h1-4，7-8，11-16，25-28H，5-6H2，(H，31，32)(H，33，34)(H，35，36)(H，37，38)(H，19，23，29)(H，20，24，30);;;;/q;4*+1/p-4/t7-，8-，11-，12-，13-，14-，15-，16-;;;;/m1..../s1 |
| PubChem CID |
148196 |
| 靶点 |
P2Y Receptor |
| 通路 |
GPCR & G Protein |
| 背景说明 |
Diquafosol tetrasodium是一种P2Y2受体激动剂。 |
| 生物活性 |
Diquafosol tetrasodium is a P2Y2 receptor agonist that stimulates fluid and mucin secretion on the ocular surface， as a topical treatment of dry eye disease.[1-3] |
| In Vitro |
在用 30% 稀释的 Diquafosol tetrasodium 处理 1 小时和用 10% 和 20% 稀释的 Diquafosol tetrasodium 处理后 6 小时后，细胞活力显著降低。单层细胞受伤 24 小时后，3% Diquafosol tetrasodium 和 0.3% HCEC 的伤口愈合明显优于对照组[1]。 |
| In Vivo |
在大鼠干眼模型中，发现 P2Y2 激动剂地夸磷索四钠可改善表面健康，其基础是增加泪液分泌、角膜上皮抵抗力和从杯状细胞中释放含糖蛋白的部分。从第 2 周开始并持续另外 2 周，Diquafosol tetrasodium 的剂量低至 1% 时，染料外显率最大下降约 50%[2]。Diquafosol tetrasodium 在浓度超过 0.1% w/v 时可显著抑制角膜损伤[3]。 |
| 细胞实验 |
The viabilities of human corneal epithelial cells (HCECs) are determined using a MTT assay. Cells are subconfluent Diquafosol (100 mL diluted 10%， 20%， or 30%) or DMEM (100 mL) is added to controls. After 1， 6， and 24 h， plates are washed three times with PBS to remove the drugs. Cell viabilities are evaluated after incubating for 24 h. MTT is then added to each well. Samples are incubated in the dark for 4 h at 37oC， and media are then removed. Precipitates are resuspended in DMSO. Absorbances are measured on a plate reader at 570 nm[1]. |
| 动物实验 |
Rats: An SD rat dry eye model is 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， INS365-containing eye drops are applied six times daily for the next 4 weeks at concentrations from 0.03% to 3.0%. Corneal barrier function is 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 is evaluated in histologic sections of the tarsal and bulbar conjunctiva[2]. |
| 数据来源文献 |
[1]. Lee JH， et al. Comparison of cytotoxicities and wound healing effects of diquafosol tetrasodium and hyaluronic acid on human corneal epithelial cells. Korean J Physiol Pharmacol. 2017 Mar;21(2):189-195.
[2]. Fujihara T， et al. Improvement of corneal barrier function by the P2Y(2) agonist INS365 in a rat dry eye model. Invest Ophthalmol Vis Sci. 2001 Jan;42(1):96-100.
[3]. Fujihara T， et al. INS365 suppresses loss of corneal epithelial integrity by secretion of mucin-like glycoprotein in a rabbit short-term dry eye model. J Ocul Pharmacol Ther. 2002 Aug;18(4):363-70. |
| 规格 |
1mg 5mg 10mg 25mg 50mg 100mg |
| 单位 |
瓶 |
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