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INS 365

Product Name
INS 365
CAS No.
211427-08-6
Chemical Name
INS 365
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
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INS 365 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
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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.

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N-Bromosuccinimide Price

ChemScene
Product number
CS-6370
Product name
Diquafosoltetrasodium
Purity
>99.0%
Packaging
5mg
Price
$96
Updated
2021/12/16
ChemScene
Product number
CS-6370
Product name
Diquafosoltetrasodium
Purity
>99.0%
Packaging
100mg
Price
$672
Updated
2021/12/16
Biosynth Carbosynth
Product number
FD159346
Product name
Diquafosol tetrasodium
Packaging
500mg
Price
$1500
Updated
2021/12/16
Biosynth Carbosynth
Product number
FD159346
Product name
Diquafosol tetrasodium
Packaging
1g
Price
$2000
Updated
2021/12/16
Biosynth Carbosynth
Product number
FD159346
Product name
Diquafosol tetrasodium
Packaging
2g
Price
$2500
Updated
2021/12/16
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INS 365 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.

INS 365 Preparation Products And Raw materials

Raw materials

Preparation Products

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INS 365 Suppliers

TopScience Biochemical
Tel
00852-68527855
Fax
00852-26406298
Email
info@itopbiochem.com
Country
China Hong Kong
ProdList
902
Advantage
58
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View Lastest Price from INS 365 manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
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
Guangzhou Tosun Pharmaceutical Limited
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
Zhuozhou Wenxi import and Export Co., Ltd
Product
Diquafosol 211427-08-6
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-11

211427-08-6, INS 365Related Search:


  • 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
  • 211427-08-6
  • C18H26N4O23P44Na