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MedKoo Cat#: 329011 | Name: Diquafosol Tetrasodium
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Diquafosol Tetrasodium, also known as Diquas and INS-365, is a P2Y2 purinoceptor receptor agonist that stimulates the secretion of mucins from ocular tissues Diquafosol tetrasodium improves tear film stability and visual function.

Chemical Structure

Diquafosol Tetrasodium
Diquafosol Tetrasodium
CAS#211427-08-6 (tetrasodium)

Theoretical Analysis

MedKoo Cat#: 329011

Name: Diquafosol Tetrasodium

CAS#: 211427-08-6 (tetrasodium)

Chemical Formula: C18H22N4Na4O23P4

Exact Mass: 0.0000

Molecular Weight: 878.23

Elemental Analysis: C, 24.62; H, 2.53; N, 6.38; Na, 10.47; O, 41.90; P, 14.11

Price and Availability

Size Price Availability Quantity
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
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Related CAS #
211427-08-6 (tetrasodium) 59985-21-6 (free base)
Synonym
Diquafosol Tetrasodium; Diquafosol sodium; INS-365; INS 365; NS365; Diquas
IUPAC/Chemical Name
Uridine 5'-(pentahydrogen tetraphosphate), P'''-5'ester with uridine, tetrasodium salt
InChi Key
OWTGMPPCCUSXIP-CNJHCLCISA-J
InChi Code
InChI=1S/C18H26N4O23P4.4Na/c23-9-1-3-21(17(29)19-9)15-13(27)11(25)7(41-15)5-39-46(31,32)43-48(35,36)45-49(37,38)44-47(33,34)40-6-8-12(26)14(28)16(42-8)22-4-2-10(24)20-18(22)30;;;;/h1-4,7-8,11-16,25-28H,5-6H2,(H,31,32)(H,33,34)(H,35,36)(H,37,38)(H,19,23,29)(H,20,24,30);;;;/q;4*+1/p-4/t7-,8-,11-,12-,13-,14-,15-,16+;;;;/m1..../s1
SMILES Code
O[C@H]([C@@H]([C@@H](COP(OP(OP(OP(OC[C@@H]1[C@H]([C@@H](O)[C@H](O1)N2C(NC(C=C2)=O)=O)O)([O-])=O)([O-])=O)([O-])=O)([O-])=O)O3)O)[C@@H]3N(C(N4)=O)C=CC4=O.[Na+].[Na+].[Na+].[Na+]
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Related CAS# 59985-21-6 (Diquafosol ) 211427-08-6 (Diquafosol Tetrasodium)
Product Data
Product Data
Instruction
View handling instruction
Biological target:
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 activity:
Hyperosmotic stressed HCECs demonstrated increased MUC5AC secretion and gene expression when treated with diquafosol. ERK signaling may regulate the expression levels of MUC1, MUC16, and MUC5AC induced by diquafosol in hyperosmotic stressed HCECs. Reference: Mol Vis. 2022 Jun 30;28:114-123. https://pubmed.ncbi.nlm.nih.gov/36034736/
In vivo activity:
Loss of tear volume secretion in chronic DED rats was significantly reversed by diquafosol instillation after 28 days, compared with saline treatment. The number of eyeblinks and pERK-IR neurons in the superficial laminae of Vc following hypertonic saline administration to the ocular surface was lower in diquafosol-treated chronic DED rats than in saline-treated rats. Reference: Neurosci Lett. 2023 Jan 1;792:136939. https://pubmed.ncbi.nlm.nih.gov/36341926/
Solvent mg/mL mM
Solubility
DMSO 1.0 1.14
Water 100.0 113.86
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 878.23 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Lee HJ, Yang S, Cheon EJ, Shin S, Byun YS, Kim HS, Chung SH. Diquafosol ophthalmic solution enhances mucin expression via ERK activation in human conjunctival epithelial cells with hyperosmotic stress. Mol Vis. 2022 Jun 30;28:114-123. PMID: 36034736; PMCID: PMC9352363. 2. Lee JH, Lee JS, Kim S, Lee JE. 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. doi: 10.4196/kjpp.2017.21.2.189. Epub 2017 Feb 21. PMID: 28280412; PMCID: PMC5343052. 3. Katagiri A, Tsubota K, Mikuzuki L, Nakamura S, Toyofuku A, Kato T, Bereiter DA, Iwata K. Diquafosol sodium reduces neuronal activity in trigeminal subnucleus caudalis in a rat model of chronic dry eye disease. Neurosci Lett. 2023 Jan 1;792:136939. doi: 10.1016/j.neulet.2022.136939. Epub 2022 Oct 29. PMID: 36341926. 4. Endo KI, Sakamoto A, Fujisawa K. Diquafosol tetrasodium elicits total cholesterol release from rabbit meibomian gland cells via P2Y2 purinergic receptor signalling. Sci Rep. 2021 Mar 26;11(1):6989. doi: 10.1038/s41598-021-86433-6. PMID: 33772064; PMCID: PMC7997929.
In vitro protocol:
1. Lee HJ, Yang S, Cheon EJ, Shin S, Byun YS, Kim HS, Chung SH. Diquafosol ophthalmic solution enhances mucin expression via ERK activation in human conjunctival epithelial cells with hyperosmotic stress. Mol Vis. 2022 Jun 30;28:114-123. PMID: 36034736; PMCID: PMC9352363. 2. Lee JH, Lee JS, Kim S, Lee JE. 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. doi: 10.4196/kjpp.2017.21.2.189. Epub 2017 Feb 21. PMID: 28280412; PMCID: PMC5343052.
In vivo protocol:
1. Katagiri A, Tsubota K, Mikuzuki L, Nakamura S, Toyofuku A, Kato T, Bereiter DA, Iwata K. Diquafosol sodium reduces neuronal activity in trigeminal subnucleus caudalis in a rat model of chronic dry eye disease. Neurosci Lett. 2023 Jan 1;792:136939. doi: 10.1016/j.neulet.2022.136939. Epub 2022 Oct 29. PMID: 36341926. 2. Endo KI, Sakamoto A, Fujisawa K. Diquafosol tetrasodium elicits total cholesterol release from rabbit meibomian gland cells via P2Y2 purinergic receptor signalling. Sci Rep. 2021 Mar 26;11(1):6989. doi: 10.1038/s41598-021-86433-6. PMID: 33772064; PMCID: PMC7997929.
1: Fischbarg J. Diquafosol tetrasodium. Inspire/Allergan/Santen. Curr Opin Investig Drugs. 2003 Nov;4(11):1377-83. PMID: 14758778. 2: Diquafosol: DE 089, diquafosol tetrasodium, INS 365, INS 365 Ophthalmic, INS 365 Respiratory, KPY 998. Drugs R D. 2003;4(6):359-62. doi: 10.2165/00126839-200304060-00005. PMID: 14584965. 3: Bremond-Gignac D, Gicquel JJ, Chiambaretta F. Pharmacokinetic evaluation of diquafosol tetrasodium for the treatment of Sjögren's syndrome. Expert Opin Drug Metab Toxicol. 2014 Jun;10(6):905-13. doi: 10.1517/17425255.2014.915026. Epub 2014 May 6. PMID: 24797483. 4: Nichols KK, Yerxa B, Kellerman DJ. Diquafosol tetrasodium: a novel dry eye therapy. Expert Opin Investig Drugs. 2004 Jan;13(1):47-54. doi: 10.1517/13543784.13.1.47. PMID: 14680452. 5: Shigeyasu C, Hirano S, Akune Y, Yamada M. Diquafosol Tetrasodium Increases the Concentration of Mucin-like Substances in Tears of Healthy Human Subjects. Curr Eye Res. 2015 Sep;40(9):878-83. doi: 10.3109/02713683.2014.967871. Epub 2014 Oct 13. PMID: 25310688. 6: Miura M, Inomata T, Nakamura M, Sung J, Nagino K, Midorikawa-Inomata A, Zhu J, Fujimoto K, Okumura Y, Fujio K, Hirosawa K, Akasaki Y, Kuwahara M, Eguchi A, Shokirova H, Murakami A. Prevalence and Characteristics of Dry Eye Disease After Cataract Surgery: A Systematic Review and Meta-Analysis. Ophthalmol Ther. 2022 Aug;11(4):1309-1332. doi: 10.1007/s40123-022-00513-y. Epub 2022 May 9. PMID: 35534685; PMCID: PMC9253209. 7: Endo KI, Sakamoto A, Fujisawa K. Diquafosol tetrasodium elicits total cholesterol release from rabbit meibomian gland cells via P2Y2 purinergic receptor signalling. Sci Rep. 2021 Mar 26;11(1):6989. doi: 10.1038/s41598-021-86433-6. PMID: 33772064; PMCID: PMC7997929. 8: Baek J, Doh SH, Chung SK. The Effect of Topical Diquafosol Tetrasodium 3% on Dry Eye After Cataract Surgery. Curr Eye Res. 2016 Oct;41(10):1281-1285. doi: 10.3109/02713683.2015.1122813. Epub 2016 Apr 6. PMID: 27049809. 9: Kaido M, Uchino M, Kojima T, Dogru M, Tsubota K. Effects of diquafosol tetrasodium administration on visual function in short break-up time dry eye. J Ocul Pharmacol Ther. 2013 Jul-Aug;29(6):595-603. doi: 10.1089/jop.2012.0246. Epub 2013 Mar 28. PMID: 23537148. 10: Eom Y, Song JS, Kim HM. Effectiveness of Topical Cyclosporin A 0.1%, Diquafosol Tetrasodium 3%, and Their Combination, in Dry Eye Disease. J Ocul Pharmacol Ther. 2022 Dec;38(10):682-694. doi: 10.1089/jop.2022.0031. PMID: 36473191. 11: Toda I, Ide T, Fukumoto T, Ichihashi Y, Tsubota K. Combination therapy with diquafosol tetrasodium and sodium hyaluronate in patients with dry eye after laser in situ keratomileusis. Am J Ophthalmol. 2014 Mar;157(3):616-22.e1. doi: 10.1016/j.ajo.2013.11.017. Epub 2013 Nov 27. PMID: 24528935. 12: Doctor MB, Basu S. Lacrimal Gland Insufficiency in Aqueous Deficiency Dry Eye Disease: Recent Advances in Pathogenesis, Diagnosis, and Treatment. Semin Ophthalmol. 2022 Oct-Nov;37(7-8):801-812. doi: 10.1080/08820538.2022.2075706. Epub 2022 May 19. PMID: 35587465. 13: Lee JH, Lee JS, Kim S, Lee JE. 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. doi: 10.4196/kjpp.2017.21.2.189. Epub 2017 Feb 21. PMID: 28280412; PMCID: PMC5343052. 14: Wang T, Di Y, Li Y. Combination therapy with 3% diquafosol tetrasodium ophthalmic solution and sodium hyaluronate: an effective therapy for patients with dry eye after femtosecond laser-assisted in situ keratomileusis. Front Med (Lausanne). 2023 Apr 20;10:1160499. doi: 10.3389/fmed.2023.1160499. PMID: 37153094; PMCID: PMC10157480. 15: Molecule of the month. Diquafosol tetrasodium. Drug News Perspect. 2003 Oct;16(8):539. PMID: 14668951. 16: Kamiya K, Nakanishi M, Ishii R, Kobashi H, Igarashi A, Sato N, Shimizu K. Clinical evaluation of the additive effect of diquafosol tetrasodium on sodium hyaluronate monotherapy in patients with dry eye syndrome: a prospective, randomized, multicenter study. Eye (Lond). 2012 Oct;26(10):1363-8. doi: 10.1038/eye.2012.166. Epub 2012 Aug 10. PMID: 22878452; PMCID: PMC3470059. 17: Tauber J, Davitt WF, Bokosky JE, Nichols KK, Yerxa BR, Schaberg AE, LaVange LM, Mills-Wilson MC, Kellerman DJ. Double-masked, placebo-controlled safety and efficacy trial of diquafosol tetrasodium (INS365) ophthalmic solution for the treatment of dry eye. Cornea. 2004 Nov;23(8):784-92. doi: 10.1097/01.ico.0000133993.14768.a9. Erratum in: Cornea. 2007 May;26(4):514. PMID: 15502479. 18: Cui L, Li Y, Lee HS, Yang JM, Choi W, Yoon KC. Effect of diquafosol tetrasodium 3% on the conjunctival surface and clinical findings after cataract surgery in patients with dry eye. Int Ophthalmol. 2018 Oct;38(5):2021-2030. doi: 10.1007/s10792-017-0693-1. Epub 2017 Aug 18. PMID: 28822028. 19: Choi KE, Song JS, Kang B, Eom Y, Kim HM. Immediate Effect of 3% Diquafosol Ophthalmic Solution on Tear MUC5AC Concentration and Corneal Wetting Ability in Normal and Experimental Keratoconjunctivitis Sicca Rat Models. Curr Eye Res. 2017 May;42(5):666-671. doi: 10.1080/02713683.2016.1233986. Epub 2016 Oct 28. PMID: 27791390. 20: Lee HJ, Yang S, Cheon EJ, Shin S, Byun YS, Kim HS, Chung SH. Diquafosol ophthalmic solution enhances mucin expression via ERK activation in human conjunctival epithelial cells with hyperosmotic stress. Mol Vis. 2022 Jun 30;28:114-123. PMID: 36034736; PMCID: PMC9352363.