Diquafosol Tetrasodium
- Product Name
- 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
- Formula Weight
- 814.3
- MOL File
- 211427-08-6.mol
Diquafosol Tetrasodium Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H228Flammable solid
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P210Keep away from heat/sparks/open flames/hot surfaces. — No smoking.
P240Ground/bond container and receiving equipment.
P241Use explosion-proof electrical/ventilating/lighting/…/equipment.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P370+P378In case of fire: Use … for extinction.
N-Bromosuccinimide Price
- Product number
- CS-6370
- Product name
- Diquafosoltetrasodium
- Purity
- >99.0%
- Packaging
- 100mg
- Price
- $672
- Updated
- 2021/12/16
- Product number
- FD159346
- Product name
- Diquafosol tetrasodium
- Packaging
- 500mg
- Price
- $1500
- Updated
- 2021/12/16
- Product number
- FD159346
- Product name
- Diquafosol tetrasodium
- Packaging
- 1g
- Price
- $2000
- Updated
- 2021/12/16
- Product number
- FD159346
- Product name
- Diquafosol tetrasodium
- Packaging
- 2g
- Price
- $2500
- Updated
- 2021/12/16
- Product number
- FD159346
- Product name
- Diquafosol tetrasodium
- Packaging
- 5G
- Price
- $3500
- Updated
- 2021/12/16
Diquafosol Tetrasodium Chemical Properties,Usage,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.
Diquafosol Tetrasodium Preparation Products And Raw materials
Raw materials
Preparation Products
Diquafosol Tetrasodium Suppliers
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View Lastest Price from Diquafosol Tetrasodium manufacturers
- Product
- Diquafosol Impurity 11 211427-08-6
- Price
- US $0.00-0.00/mg
- Min. Order
- 5mg
- Purity
- 95%+
- Supply Ability
- 1000mg
- Release date
- 2025-02-12
- Product
- Diquafosol Sodium 211427-08-6
- Price
- US $0.00/KG
- Min. Order
- 1KG
- Purity
- 99%min
- Supply Ability
- 10kg
- Release date
- 2021-09-13
- Product
- Diquafosol Impurity 11 211427-08-6
- Price
- US $0.00/mg
- Min. Order
- 1mg
- Purity
- 99.88%
- Supply Ability
- 50mg
- Release date
- 2023-06-27