Diquafosol tetrasodium

SKU: orb1299832

Description

Diquafosol tetrasodium

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 211427-08-6
• MW: 878.23
• Purity: 98.70%
• Formula: C₁₈H₂₂N₄Na₄O₂₃P₄
• SMILES: O=c1ccn(C2OC(COP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OP(=O)([O-])OCC3OC(n4ccc(=O)[nH]c4=O)C(O)C3O)C(O)C2O)c(=O)[nH]1.[Na+].[Na+].[Na+].[Na+]
• Target: P2Y Receptor
• Solubility: DMSO:Insoluble;H2O:247.5 mg/mL (281.82 mM)

Bioactivity

• In Vivo:
  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 syndrom.
• In Vitro:
  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 observe.
• Cell Research:
  The viability of human corneal epithelial cells (HCECs) was determined using an MTT assay. Cells (100 μL; 1 × 10⁴ cells/mL) were plated in 96‑well tissue‑culture plates and incubated at 37 °C in 5% CO₂ for 24 to 48 h until cultures were subconfluent. Diquafosol (100 μL diluted to 10%, 20%, or 30%) or 0.3% or 0.18% HA was 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 viability was 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 °C, and media were then removed. Precipitates were resuspended in dimethyl sulfoxide (100 μL; DMSO, Sigma‑Aldrich). Absorbances were measured on a plate reader at 570 nm. The experiment was performed in triplicate.
• Animal Research:
  An SD rat dry eye model was used in which exorbital lacrimal g and extirpation decrease 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 fo the Next 4 weeks at concentration 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 o the tarsal and bulbar conjunctiv.

Storage & Handling

• Storage: keep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Diquafosol, Diquafosol tetrasodium, inhibit, Inhibitor, INS 365, INS365, INS-365, P2Y, P2YReceptor, P2Y Receptor, P2Y2 receptor

Compound Identifiers

PubChem CID

137795696