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Diquafosol tetrasodium

Catalog No. T7423   CAS 211427-08-6
Synonyms: INS365

Diquafosol Tetrasodium is a P2Y2 receptor agonist that stimulates the secretion of mucins from ocular tissues Diquafosol tetrasodium (INS365) improves tear film stability and visual function, as a topical treatment of dry eye disease.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Diquafosol tetrasodium Chemical Structure
Diquafosol tetrasodium, CAS 211427-08-6
Pack Size Availability Price/USD Quantity
2 mg In stock $ 39.00
5 mg In stock $ 64.00
10 mg In stock $ 97.00
25 mg In stock $ 192.00
50 mg In stock $ 328.00
100 mg In stock $ 495.00
500 mg In stock $ 1,080.00
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Purity: 99.68%
Purity: 98.7%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Diquafosol Tetrasodium is a P2Y2 receptor agonist that stimulates the secretion of mucins from ocular tissues Diquafosol tetrasodium (INS365) improves tear film stability and visual function, as a topical treatment of dry eye disease.
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 observed[1].
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 syndrome[2].
Cell Research The viabilities of human corneal epithelial cells (HCECs) were determined using a MTT assay.?Cells (100 μl;?5×104 cell/mL) were plated in 96-well tissue-culture plates and incubated at 37℃ in 5% CO2 for 24 to 48 h until cultures were subconfluent.?Diquafosol (100 μl diluted 10%, 20%, or 30%) or 0.3% or 0.18% HA were 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 viabilities were 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℃, and media were then removed.?Precipitates were resuspended indimethyl sulfoxide (100 μl;?DMSO, Sigma-Aldrich).?Absorbances were measured on a plate reader at 570 nm.?The experiment was performed in triplicate[1].
Animal Research An SD rat dry eye model was 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, Diquafosol tetrasodium(INS365)-containing eye drops were applied six times daily for the next 4 weeks at concentrations 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 of the tarsal and bulbar conjunctiva[2].
Synonyms INS365
Molecular Weight 878.23
Formula C18H22N4Na4O23P4
CAS No. 211427-08-6

Storage

keep away from direct sunlight,store under nitrogen

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 10 mM

DMSO: Insoluble

TargetMolReferences and Literature

1. Lee J H , Lee J S , Kim S , et al. Comparison of cytotoxicities and wound healing effects of diquafosol tetrasodium and hyaluronic acid on Human corneal epithelial cells[J]. Korean Journal of Physiology and Pharmacology, 2017, 21(2):189. 2. Fujihara T , Murakami T , Fujita H , et al. Improvement of Corneal Barrier Function by the P2Y2 Agonist INS365 in a Rat Dry Eye Model[J]. Investigative Ophthalmology & Visual Science, 2001, 42(1):96-100.

TargetMolCitations

1. Zhao Y, Li Y, Zhu R, et al.RPS15 interacted with IGF2BP1 to promote esophageal squamous cell carcinoma development via recognizing m6A modification.Signal Transduction and Targeted Therapy.2023, 8(1): 224.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Drug Repurposing Compound Library GPCR Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Clinical Compound Library Anti-COVID-19 Compound Library Anti-Cancer Compound Library Anti-Infection Compound Library Approved Drug Library

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Keywords

Diquafosol tetrasodium 211427-08-6 GPCR/G Protein Neuroscience P2Y Receptor Inhibitor inhibit INS 365 Diquafosol INS-365 INS365 inhibitor

 

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