Diquafosol tetrasodium

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.

Product information

CAS Number: 211427-08-6

Molecular Weight: 878.23

Formula: C18H22N4Na4O23P4

Chemical Name: tetrasodium [(2R,3S,4R,5R)-5-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methyl [({[({[(2R,3S,4R,5R)-5-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methyl phosphonato}oxy)(oxido)phosphoryl]oxy}(oxido)phosphoryl)oxy]phosphonate

Smiles: [Na+].[Na+].[Na+].[Na+].[O-]P(=O)(OP([O-])(=O)OP([O-])(=O)OC[C@H]1O[C@H]([C@H](O)[C@@H]1O)N1C=CC(=O)NC1=O)OP([O-])(=O)OC[C@H]1O[C@H]([C@H](O)[C@@H]1O)N1C=CC(=O)NC1=O

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 1 mg/mL (1.14 mM; Need ultrasonic). H2O : 100 mg/mL (113.87 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Cell viability significantly decreased after treatment with 30% diluted diquafosol for 1 hour and 6 hours after treatment with 10% and 20% diluted diquafosol. Twenty-four hours after wounding monolayers, 3% diquafosol, and 0.3% HCECs exhibits significantly more wound healing than the control.

In Vivo:

In a rat dry eye model, the P2Y2 agonist diquafosol tetrasodium is found to improve surface health, based on increases in tear fluid secretion, corneal epithelial resistance, and release of glycoprotein-containing moieties from goblet cells. Beginning at 2 weeks and continuing for an additional 2 weeks, maximal declines in dye penetrance of approximately 50% occurred with doses of diquafosol tetrasodium as low as 1%. INS365 significantly suppresses corneal damage at concentrations of more than 0.1% w/v.

Products are for research use only. Not for human use.