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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Diquafosol tetrasodium (Diquas; INS-365) is a novel and potent P2Y2 purinoceptor agonist that stimulates fluid and mucin secretion on the ocular surface, and is used as a topical treatment of dry eye disease.
| Targets |
P2Y2 receptor
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|---|---|
| ln Vitro |
Cell viability was significantly reduced after treatment with 30% diquafosol tetrasodium for 1 hour and 10% and 20% diquafosol tetrasodium for 6 hours. 24 hours after monolayer cell damage, wound healing was significantly aggravated by 3% diquafosol tetrasodium and 0.3% HCEC [1].
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| ln Vivo |
In a mini-dry eye model, the P2Y2 agonist tetraphosphonate was found to restore surface health based on increased tear production, corneal epithelial resistance, and the release of glycoproteins from goblet cells. Beginning in week 2 and continuing for 2 weeks, the maximum decrease in dye-extrasigma rate was approximately 50% at doses as low as 1% of diquafosol tetrasodium [2]. Diquafosol tetrasodium can significantly interfere with potential damage when the concentration exceeds 0.1% w/v [3].
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| Cell Assay |
The MTT assay is used to assess the viability of human corneal epithelial cells (HCECs). Diquafosol (100%, 20%, or 30% diluted) or DMEM (100 mL) is added to controls when the cells are subconfluent. To get rid of the medications, plates are cleaned three times using PBS after one, six, and twenty-four hours. After a 24-hour incubation period, cell viability is assessed. Next, each well receives an addition of MTT. After 4 hours of dark incubation at 37°C, the samples are removed from the media. The precipitates are reconstituted in DMSO. At 570 nm, absorbances are measured using a plate reader[1].
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| Animal Protocol |
Rats: The Schirmer test score was at least 50% lower in an SD rat dry eye model after exorbital lacrimal gland extraction. INS365-containing eye drops are administered six times a day for the following four weeks at concentrations ranging from 0.03% to 3.0% after eight weeks, at which point there have been noticeable increases in corneal epithelial permeability. Measurements of fluorescein penetrance obtained with a modified anterior fluorometer at 1, 2, and 4 weeks following initial application are used to assess the function of the corneal barrier. The periodic acid-Schiff reagent (PAS)-stained area is assessed in histologic sections of the bulbar and tarsal conjunctiva following INS365 application[2].
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| References |
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| Molecular Formula |
C18H22N4NA4O23P4
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|---|---|
| Molecular Weight |
878.234680000001
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| Exact Mass |
877.92
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| Elemental Analysis |
C, 24.62; H, 2.53; N, 6.38; Na, 10.47; O, 41.90; P, 14.11
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| CAS # |
211427-08-6
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| Related CAS # |
211427-08-6 (tetrasodium); 59985-21-6
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| Appearance |
Solid powder
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| SMILES |
C1=CN(C(=O)NC1=O)[C@H]2[C@@H]([C@@H]([C@H](O2)COP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OC[C@@H]3[C@H]([C@H]([C@@H](O3)N4C=CC(=O)NC4=O)O)O)O)O.[Na+].[Na+].[Na+].[Na+]
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| InChi Key |
OWTGMPPCCUSXIP-FNXFGIETSA-J
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| InChi Code |
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
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| Chemical Name |
tetrasodium;[[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl] [[[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl]oxy-oxidophosphoryl] phosphate
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| Synonyms |
INS-365; DE-089; KPY-998; INS 365; DE 089; KPY 998; INS365; DE089; KPY998; Diquas
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: ~100 mg/mL (~113.9 mM)
DMSO: ~1 mg/mL (~1.1 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (113.87 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05682547 | Not yet recruiting | Drug: 3% Diquafosol tetrasodium Drug: 0.1% hyaluronate |
Diabetic Eye Problems | He Eye Hospital | November 1, 2023 | Not Applicable |
| NCT05193331 | Not yet recruiting | Drug: 3% Diquafosol tetrasodium | Diabetic Eye Problems | He Eye Hospital | April 1, 2023 | Not Applicable |
| NCT04980144 | Recruiting | Drug: 3% Diquafosol tetrasodium Drug: 0.1% hyaluronate |
Diabetic Eye Problems | He Eye Hospital | March 3, 2023 | Not Applicable |
| NCT05720754 | Not yet recruiting | Drug: Diquafosol tetrasodium Device: Heated eye mask |
Dry Eye | He Eye Hospital | April 2, 2023 | Not Applicable |
| NCT05694026 | Completed | Device: Intense pulsed light Drug: Diquafosol tetrasodium |
Dry Eye | He Eye Hospital | March 1, 2023 | Not Applicable |
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