1. GPCR/G Protein
  2. P2Y Receptor

Diquafosol tetrasodium (Synonyms: INS365)

Cat. No.: HY-B0606 Purity: 99.93%
Handling Instructions

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.

For research use only. We do not sell to patients.

Diquafosol tetrasodium Chemical Structure

Diquafosol tetrasodium Chemical Structure

CAS No. : 211427-08-6

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Estimated Time of Arrival: December 31
50 mg USD 432 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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.

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[1].

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%[2]. INS365 significantly suppresses corneal damage at concentrations of more than 0.1% w/v[3].

Clinical Trial
Solvent & Solubility
In Vitro: 

H2O : ≥ 32 mg/mL (36.44 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

878.23

Formula

C₁₈H₂₂N₄Na₄O₂₃P₄

CAS No.

211427-08-6

SMILES

O[[email protected]]1[[email protected]](N(C=CC2=O)C(N2)=O)O[[email protected]](COP(OP(OP(OP(OC[[email protected]]3O[[email protected]@H](N(C=CC4=O)C(N4)=O)[[email protected]](O)[[email protected]@H]3O)([O-])=O)([O-])=O)([O-])=O)([O-])=O)[[email protected]]1O.[Na+].[Na+].[Na+].[Na+]

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.93%

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Product Name:
Diquafosol tetrasodium
Cat. No.:
HY-B0606
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Diquafosol tetrasodium

Cat. No.: HY-B0606