Diquafosol tetrasodium (INS365)
(Synonyms: 地夸磷索四钠; INS365) 目录号 : GC31664
A P2Y2 and P2Y4 receptor agonist
Cas No.:211427-08-6
Sample solution is provided at 25 µL, 10mM.
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Diquafosol is an agonist of purinergic P2Y2 and P2Y4 receptors (EC50s = 0.1 and 0.4 ?M, respectively, in calcium mobilization assays).1 It is selective for P2Y2 and P2Y4 receptors over P2Y6 receptors (EC50 = 20 ?M). Ocular application of diquafosol (0.1 and 1% w/v) induces the release of mucin-like glycoproteins from rabbit conjunctival goblet cells, as well as reduces desiccation-induced corneal damage in a rabbit model of dry eye disease.2 Formulations containing diquafosol have been used in the treatment of dry eye disease.
1.Pendergast, W., Yerxa, B.R., Douglass, J.G., III, et al.Synthesis and P2Y receptor activity of a series of uridine dinucleoside 5'-polyphosphatesBioorg. Med. Chem. Lett.11(2)157-160(2001) 2.Fujihara, T., Murakami, T., Nagano, T., et al.INS365 suppresses loss of corneal epithelial integrity by secretion of mucin-like glycoprotein in a rabbit short-term dry eye modelJ. Ocul. Pharmacol. Ther.18(4)363-370(2002)
Cell experiment: | 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]. |
Animal experiment: | 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]. |
References: [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. | |
| Cas No. | 211427-08-6 | SDF | |
| 别名 | 地夸磷索四钠; INS365 | ||
| Canonical SMILES | O[C@H]1[C@H](N(C=CC2=O)C(N2)=O)O[C@H](COP(OP(OP(OP(OC[C@H]3O[C@@H](N(C=CC4=O)C(N4)=O)[C@H](O)[C@@H]3O)([O-])=O)([O-])=O)([O-])=O)([O-])=O)[C@H]1O.[Na+].[Na+].[Na+].[Na+] | ||
| 分子式 | C18H22N4Na4O23P4 | 分子量 | 878.23 |
| 溶解度 | Water : ≥ 32 mg/mL (36.44 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.1387 mL | 5.6933 mL | 11.3865 mL |
| 5 mM | 0.2277 mL | 1.1387 mL | 2.2773 mL |
| 10 mM | 0.1139 mL | 0.5693 mL | 1.1387 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet