[CAS NO. 211427-08-6] Diquafosol tetrasodium
PRODUCTS SPECIFICATIONS [211427-08-6]
DESCRIPTION [211427-08-6]
Overview
| MDL | MFCD18071356 |
|---|---|
| Molecular Weight | 878.23 |
| Molecular Formula | C18H22N4Na4O23P4 |
| SMILES | O[C@H]1[C@@H](O)[C@H](N(C(N2)=O)C=CC2=O)O[C@@H]1COP(OP(OP(OP(OC[C@@H]3[C@@H](O)[C@@H](O)[C@H](N4C(NC(C=C4)=O)=O)O3)(O[Na])=O)(O[Na])=O)(O[Na])=O)(O[Na])=O |
3 Publications Citing Use of MCE
Summary
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.
IC50 & Target
|
P2Y2 Receptor |
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00831662 | Merck Sharp & Dohme LLC |
Dry Eye Disease
|
January 2009 | Phase 3 |
| NCT00600288 | Merck Sharp & Dohme LLC |
Dry Eye Disease
|
January 2008 | Phase 3 |
| NCT04668118 | Peking University Third Hospital |
Dry Eye Syndromes|Computer Vision Syndrome|Asthenopia
|
February 1, 2021 | Phase 4 |
| NCT01101984 | Santen Pharmaceutical Co., Ltd. |
Dry Eye
|
February 2010 | Not Applicable |
| NCT05193331 | He Eye Hospital|Santen Pharmaceutical(China) Co.,LTD |
Diabetic Eye Problems
|
April 1, 2022 | Not Applicable |
| NCT05346783 | Taejoon Pharmaceutical Co., Ltd. |
Dry Eye Syndromes
|
October 14, 2021 | Phase 1|Phase 2 |
| NCT02608489 | Soonchunhyang University Hospital |
Dry Eye Syndromes
|
January 2014 | Not Applicable |
| NCT00679718 | Merck Sharp & Dohme LLC |
Dry Eye Disease
|
January 2000 | Phase 2 |
| NCT00403715 | Merck Sharp & Dohme LLC |
Dry Eye Disease
|
February 2001 | Phase 3 |
| NCT04980144 | He Eye Hospital |
Diabetic Eye Problems
|
August 1, 2021 | Not Applicable |
| NCT05383612 | Zhongshan Ophthalmic Center, Sun Yat-sen University |
Dry Eye|Meibomian Gland Dysfunction
|
August 5, 2022 | Not Applicable |
| NCT01381731 | Merck Sharp & Dohme LLC |
Photorefractive Keratectomy
|
April 2005 | Phase 2 |
| NCT00037661 | Merck Sharp & Dohme LLC |
Keratoconjunctivitis Sicca
|
April 2002 | Phase 3 |
| NCT00404131 | Merck Sharp & Dohme LLC |
Dry Eye Disease
|
March 2001 | Phase 3 |
| NCT05456061 | Yonsei University |
Tear|Dry Eye Syndromes
|
August 1, 2018 | Not Applicable |
| NCT00403975 | Merck Sharp & Dohme LLC |
Dry Eye Disease
|
June 2004 | Phase 3 |
| NCT03640351 | Yonsei University |
Dry Eye|Cataract Surgery
|
August 15, 2017 | Not Applicable |
| NCT00680108 | Merck Sharp & Dohme LLC |
Dry Eye Disease
|
September 1999 | Phase 2 |
| NCT04952987 | Mun Wai Lee|Santen Oy|LEC Eye Centre |
Dry Eye
|
January 1, 2021 | |
| NCT04548427 | Chong Kun Dang Pharmaceutical |
Dry Eye Disease
|
September 22, 2020 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 100 mg/mL ( 113.87 mM ; Need ultrasonic)
DMSO : 1 mg/mL ( 1.14 mM ; Need ultrasonic)
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 |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (113.87 mM); Clear solution; Need ultrasonic
References
- [1] Lee JH, et al. Comparison of cytotoxicities and wound healing effects of diquafosol tetrasodium and hyaluronic acid on human corneal epithelial cells. Korean J Physiol Pharmacol. 2017 Mar;21(2):189-195.
- [2] Fujihara T, et al. Improvement of corneal barrier function by the P2Y(2) agonist INS365 in a rat dry eye model. Invest Ophthalmol Vis Sci. 2001 Jan;42(1):96-100.
- [3] Fujihara T, et al. INS365 suppresses loss of corneal epithelial integrity by secretion of mucin-like glycoprotein in a rabbit short-term dry eye model. J Ocul Pharmacol Ther. 2002 Aug;18(4):363-70.