INS 365
- CAS No.
- 211427-08-6
- Chemical Name:
- INS 365
- Synonyms
- D03864;INS 365;Diquafosol sodium;Diquafosol tetrasodium;Diquafosol sodium (jan);Dexamethoxol tetrasodium;Diquafosol Tetrasodium CRS;Diquafosol Tetrasodium Salt;Diquafosol Impurity 7(UP4U);Diquafosol tetrasodium (usan)
- CBNumber:
- CB41347117
- Molecular Formula:
- C18H27N4NaO23P4
- Molecular Weight:
- 814.3
- MDL Number:
- MFCD18071356
- MOL File:
- 211427-08-6.mol
| 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 |
| FDA UNII | X8T9SBH9LL |
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 |
|
INS 365 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 |
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.
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.
INS 365 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Guangzhou Tosun Pharmaceutical Limited | +8618922120635 | sales@toref-standards.com | China | 1000 | 58 |
| Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 | info@tianfuchem.com | China | 21691 | 55 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 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 | 14336 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| TopScience Biochemical | 00852-68527855 | info@itopbiochem.com | China Hong Kong | 902 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| Hubei Ipure Biology Co., Ltd | +8613367258412 | ada@ipurechemical.com | China | 10326 | 58 |
| Hebei Minshang Biological Technology Co. LTD | +8618132649059 18132649059 | monica@hbminshang.cn | CHINA | 203 | 58 |
View Lastest Price from INS 365 manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2024-04-11 | Diquafosol Impurity 11
211427-08-6
|
US $0.00 / mg | 1mg | 99.88% | 50mg | Guangzhou Tosun Pharmaceutical Limited | |
 |
2023-04-12 | INS 365
211427-08-6
|
US $1.00 / kg | 1kg | above 99% | 3000tons/year | Wuhan Dujiang Industrial Co., Ltd. | |
 |
2021-09-29 | Diquafosol Sodium
211427-08-6
|
US $0.00 / KG | 1KG | 99%min | 10kg | WUHAN FORTUNA CHEMICAL CO., LTD |
-
- Diquafosol Impurity 11
211427-08-6
- US $0.00 / mg
- 99.88%
- Guangzhou Tosun Pharmaceutical Limited
-
- INS 365
211427-08-6
- US $1.00 / kg
- above 99%
- Wuhan Dujiang Industrial Co., Ltd.
-
- Diquafosol Sodium
211427-08-6
- US $0.00 / KG
- 99%min
- WUHAN FORTUNA CHEMICAL CO., LTD