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Diquafosol Tetrasodium

CAS No.
211427-08-6
Chemical Name:
Diquafosol Tetrasodium
Synonyms
D03864;INS 365;CID 9876095;Diquafosol sodium;Diquafosoftetrasodium;Diquafosol tetrasodium;Diquafosol sodium (jan);Dexamethoxol tetrasodium;Diquafosol Tetrasodium CRS;Diquafosol Tetrasodium Salt
CBNumber:
CB41347117
Molecular Formula:
C18H27N4NaO23P4
Molecular Weight:
814.3
MDL Number:
MFCD18071356
MOL File:
211427-08-6.mol
Last updated:2025-02-12 13:10:04

Diquafosol Tetrasodium Properties

storage temp. Store at -20°C
solubility DMSO:1.0(Max Conc. mg/mL);1.14(Max Conc. mM)
Water:100.0(Max Conc. mg/mL);113.86(Max Conc. mM)
form A solid
color White to off-white
optical activity [α]/D -12.0 to -8.0°, c =1.0 in H2O
Water Solubility H2O: 2mg/mL, clear
InChIKey XPZQVLUPTGTIJP-NIBQMMLDNA-N
FDA UNII X8T9SBH9LL
UNSPSC Code 12352200
NACRES NA.77

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictogramsGHS hazard pictograms
GHS07,GHS02
Signal word  Warning
Hazard statements  H315-H319-H228
Precautionary statements  P240-P210-P241-P264-P280-P302+P352-P370+P378-P337+P313-P305+P351+P338-P362+P364-P332+P313
NFPA 704
0
2 0

Diquafosol Tetrasodium price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
ChemScene CS-6370 Diquafosoltetrasodium >99.0% 211427-08-6 100mg $672 2021-12-16 Buy
Biosynth Carbosynth FD159346 Diquafosol tetrasodium 211427-08-6 500mg $1500 2021-12-16 Buy
Biosynth Carbosynth FD159346 Diquafosol tetrasodium 211427-08-6 1g $2000 2021-12-16 Buy
Biosynth Carbosynth FD159346 Diquafosol tetrasodium 211427-08-6 2g $2500 2021-12-16 Buy
Biosynth Carbosynth FD159346 Diquafosol tetrasodium 211427-08-6 5G $3500 2021-12-16 Buy
Product number Packaging Price Buy
CS-6370 100mg $672 Buy
FD159346 500mg $1500 Buy
FD159346 1g $2000 Buy
FD159346 2g $2500 Buy
FD159346 5G $3500 Buy

Diquafosol Tetrasodium Chemical Properties,Uses,Production

Description

Diquafosol (INS-365) was approved in Japan in 2010 as a 3% ophthalmic solution for treatment of dry eye disease. Clinical diagnosis of dry eye is difficult because the condition presents a variety of symptoms. Treatment options include tear supplements (lubricants), anti-inflammatory drugs (e.g., cyclosporine eye drops or steroid eye drops), and tear retention devices. Diquafosol is a unique agent for the treatment of dry eye in that it acts as a P2Y2 purinergic receptor agonist with the ability to activate this receptor on the ocular surface and stimulate water, lipid, and mucin secretion. Diquafosol is metabolized by phosphodiesterases to UTP, UDP, UMP, and uridine. Diquafosol has been well tolerated in clinical trials, with side effects being local to the ocular surface.In addition,no serious ocular or systemic adverse drug reactions were found during the clinical trials.

Originator

Inspire Pharmaceuticals (United States)

Uses

Enhancement of mucosal hydration in the treatment of chronic dry eye (P2Y2 receptor antagonist).

brand name

Diquas

Clinical Use

Diquafosol tetrasodium was approved in April 2010 as Diquas ® ophthalmic solution 3% for the treatment of dry eye syndrome and launched in Japan by Santen Pharmaceuticals. Diquafosol tetrasodium was originally discovered by Inspire Pharmaceuticals. In 2001, it was licensed to Santen for co-development and commercialization in Asian countries, and co-developed in collaboration with Allergan for the countries outside of Asia. In the U.S., diquafosol tetrasodium was submitted for a New Drug Application (NDA) as Prolacria ®(2% ophthalmic formulation) in June 2003. However, it is still in Phase III clinical development for dry eye syndrome. Diquafosol tetrasodium, also known as INS- 365, is a P2Y2 receptor agonist, which activates P2Y2 receptor on the ocular surface, leading to rehydration through activation of the fluid pump mechanism of the accessory lacrimal glands on the conjunctival surface.

Synthesis

The large-scale synthesis route of diquafosol tetrasodium is described in Scheme 4. Commercially available uridine 5?ˉ-diphosphate disodium salt (21) was transformed into the corresponding tributylamine salt by ion exchange chromatography on Dowex 50 using Bu3NH+ phase, and then dimerized by means of CDI in DMF at 50 oC. The crude product was purified by Sephadex DEAE column followed by ion exchange using a Dowex 50W resin in Na+ mode. The onepot process provided diquafosol tetrasodium (IV) in 25% yield.

Synthesis_211427-08-6

Diquafosol Tetrasodium Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 173)Suppliers
Supplier Tel Email Country ProdList Advantage
Guangzhou Tosun Pharmaceutical Limited
+8618922120635 sales@toref-standards.com China 998 58
Guangzhou Tosun Pharmaceutical Ltd
+86-020-61855200-902 +8618124244216 info@upharm.cn China 897 58
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512 info@tianfuchem.com China 21628 55
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 33024 60
Jinan Chenghui-Shuangda Chemical Co.,Ltd
+86-531-58897082 ericqiao@jnchsd.com CHINA 158 58
Standardpharm Co. Ltd.
86-714-3992388 overseasales1@yongstandards.com United States 14332 58
BOC Sciences
+1-631-485-4226 inquiry@bocsci.com United States 19552 58
TopScience Biochemical
00852-68527855 info@itopbiochem.com China Hong Kong 902 58
career henan chemical co
+86-0371-86658258 +8613203830695 factory@coreychem.com China 29807 58
Hubei Ipure Biology Co., Ltd
+8613367258412 ada@ipurechemical.com China 10244 58

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View Lastest Price from Diquafosol Tetrasodium manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Diquafosol Sodium pictures 2025-05-14 Diquafosol Sodium
211427-08-6
US $0.00 / KG 1KG 99%min 10kg WUHAN FORTUNA CHEMICAL CO., LTD
Diquafosol Impurity 11 pictures 2025-05-06 Diquafosol Impurity 11
211427-08-6
US $0.00-0.00 / mg 5mg 95%+ 1000mg Guangzhou Tosun Pharmaceutical Ltd
Diquafosol Impurity 11 pictures 2024-04-11 Diquafosol Impurity 11
211427-08-6
US $0.00 / mg 1mg 99.88% 50mg Guangzhou Tosun Pharmaceutical Limited

Diquafosol Tetrasodium Spectrum

INS 365 D03864 Diquafosol sodium Diquafosol sodium (jan) Diquafosol tetrasodium Diquafosol tetrasodium (usan) Diquafosol Impurity 7(UP4U) [[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl] [[[(2R,3S,4R,5R)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-oxidophosphoryl]oxy-oxidophosphoryl] phosphate Diquafosol Tetrasoudium or P1,P4-Di(Uridine-5′-Tetraphosphate) Diquafosol Tetrasodium Salt Diquafosol tetrasodium impurity Diquafosol tetrasodium intermediate P1,P4-Diuridine 5'-tetraphosphate tetrasodium salt Diquafosol Tetrasodium (INS365) Diquafosol Sodium Reference Substance TIANFUCHEM--211427-08-6 INS 365 Dexamethoxol tetrasodium Diquafosol Tetrasodium CRS Diquafosoftetrasodium CID 9876095 Uridine 5′-(pentahydrogen tetraphosphate), P′′′→5′-ester with uridine, sodium salt (1:4) 211427-08-6 C18H26N4O23P44Na