INS 365

INS 365 Structure
CAS No.
211427-08-6
Chemical Name:
INS 365
Synonyms
D03864;INS 365;Diquafosol sodium;Diquafosoftetrasodium;Diquafosol tetrasodium;Diquafosol sodium (jan);Dexamethoxol tetrasodium;Diquafosol Tetrasodium CRS;Diquafosol Tetrasodium Salt;Diquafosol Impurity 7(UP4U)
CBNumber:
CB41347117
Molecular Formula:
C18H27N4NaO23P4
Molecular Weight:
814.3
MOL File:
211427-08-6.mol
Modify Date:
2024/7/2 8:55:07

INS 365 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

SAFETY

Risk and Safety Statements

Symbol(GHS) 
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

INS 365 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.

Uses

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

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.

INS 365 Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 158)Suppliers
Supplier Tel Country ProdList Advantage Inquiry
Pharma Affiliates 172-5066494 Haryana, India 6761 58 Inquiry
CLEARSYNTH LABS LTD. +91-22-45045900 Hyderabad, India 6351 58 Inquiry
Pharmaffiliates Analytics and Synthetics P. Ltd +91-172-5066494 Haryana, India 6773 58 Inquiry
Guangzhou Tosun Pharmaceutical Limited +8618922120635 China 1000 58 Inquiry
Henan Tianfu Chemical Co.,Ltd. +86-0371-55170693 +86-19937530512 China 21667 55 Inquiry
ATK CHEMICAL COMPANY LIMITED +undefined-21-51877795 China 32836 60 Inquiry
BOC Sciences +1-631-485-4226 United States 19553 58 Inquiry
career henan chemical co +86-0371-86658258 +8613203830695 China 29824 58 Inquiry
Hubei Ipure Biology Co., Ltd +8613367258412 China 10326 58 Inquiry
ANHUI WITOP BIOTECH CO., LTD +8615255079626 China 23555 58 Inquiry

INS 365 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 intermediate P1,P4-Diuridine 5'-tetraphosphate tetrasodium salt Diquafosol tetrasodium impurity Diquafosol Tetrasodium (INS365) Diquafosol Sodium Reference Substance TIANFUCHEM--211427-08-6 INS 365 Dexamethoxol tetrasodium Diquafosol Tetrasodium CRS Diquafosoftetrasodium 211427-08-6 C18H26N4O23P44Na