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Chemical Structure| 211427-08-6 Chemical Structure| 211427-08-6

Structure of Diquafosol tetrasodium
CAS No.: 211427-08-6

Chemical Structure| 211427-08-6

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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.

Synonyms: INS365; Diquafosol (sodium salt); KPY 998

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Product Details of Diquafosol tetrasodium

CAS No. :211427-08-6
Formula : C18H22N4Na4O23P4
M.W : 878.23
SMILES Code : O[C@H]1[C@H](N2C(NC(C=C2)=O)=O)O[C@H](COP(OP(OP(OP(OC[C@H]3O[C@@H](N4C(NC(C=C4)=O)=O)[C@H](O)[C@@H]3O)([O-])=O)([O-])=O)([O-])=O)([O-])=O)[C@H]1O.[Na+].[Na+].[Na+].[Na+]
Synonyms :
INS365; Diquafosol (sodium salt); KPY 998
MDL No. :MFCD18071356

Safety of Diquafosol tetrasodium

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of Diquafosol tetrasodium

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
human corneal epithelial cells (HCECs) 1 mM 4 or 6 days Promoted MUC1 expression and impeded intracellular fluorescein ingress Invest Ophthalmol Vis Sci. 2022 Feb 1;63(2):31
Human corneal epithelial cells (HCECs) 100 µM 8 hours To evaluate the effect of Diquafosol on cell viability and wound healing under hyperosmotic stress. Results showed that Diquafosol restored cell viability, promoted wound healing, and reduced the expression of inflammation-related genes. Cells. 2024 Jul 25;13(15):1251
rabbit meibomian gland cells 0.85% 4 hours To investigate the effect of Diquafosol on total cholesterol release from rabbit meibomian gland cells, results showed that Diquafosol significantly increased total cholesterol release in a dose-dependent manner, and this effect was significantly inhibited by AR-C118925XX and the intracellular Ca2+ chelator BAPTA-AM. Sci Rep. 2021 Mar 26;11(1):6989
rabbit meibomian gland cells 0.015% to 0.85% To investigate the effect of Diquafosol on intracellular Ca2+ signaling in rabbit meibomian gland cells, results showed that Diquafosol significantly increased intracellular Ca2+ signaling in a dose-dependent manner, and this increase was almost completely inhibited by the selective P2Y2 receptor antagonist AR-C118925XX. Sci Rep. 2021 Mar 26;11(1):6989

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Environmental dry eye stress model Eye drops 3% Twice daily for 3 days To compare the therapeutic effects of 3% Diquafosol eye drops with different molecular weight hyaluronic acid eye drops in environmental dry eye stress model mice. Results showed that the DQ group did not show significant changes in tear secretion volume, but tear film breakup time (BUT) significantly decreased. Int J Mol Sci. 2020 May 15;21(10):3516
NOD.B10.H2b mice Desiccation stress-induced dry eye mouse model Topical 3% 6 times per day for 10 days To evaluate the effect of Diquafosol on dry eye symptoms including tear quantity, ocular surface stabilization, and inflammation. Results showed that Diquafosol significantly increased tear production and improved corneal epithelial stability, but had a weaker effect on suppressing inflammation in the lacrimal gland. Sci Rep. 2017 Aug 7;7(1):7413
Mice Dry eye model Eye drops 3% 6 times daily for 14 days, then 6 times daily for 22 days To evaluate the therapeutic effect of Diquafosol on dry eye, results showed that Diquafosol significantly reduced the fluorescein-stained area Ophthalmol Sci. 2023 Oct 19;4(2):100414
C57BL/6 mice Experimental dry eye model Ophthalmic instillation 0.03 6 times daily for 10 days To evaluate the therapeutic effect of Diquafosol on dry eye disease in vivo. Results showed that Diquafosol reduced corneal staining scores, increased NGF expression, and promoted corneal wound healing. Cells. 2024 Jul 25;13(15):1251

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.14mL

0.23mL

0.11mL

5.69mL

1.14mL

0.57mL

11.39mL

2.28mL

1.14mL

Dissolving Methods
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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