All Photos(1)
Synonym(s):
Diuridine 5′-tetraphosphate, sodium salt, INS365, KPY 998, P ,P -Diuridine 5′-tetraphosphate tetrasodium salt, Up4U 4Na, Uridine 5′-(pentahydrogen tetraphosphate), P′′′→5′-ester with uridine, sodium salt (1:4), Diuridine 5′-tetraphosphate, Up4U tetrasodium
Empirical Formula (Hill Notation):
C18H22N4Na4O23P4
Recommended Products
Quality Level
Assay
>95% (HPLC)
form
powder
optical activity
[α]/D -12.0 to -8.0°, c = 1.0 in H2O
color
white to beige
solubility
H2O: 2 mg/mL, clear
storage temp.
−20°C
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Biochem/physiol Actions
Diquafosol (Up4U, INS365) is a selective purinergic receptor P2Y2 agonist (EC50 = 100 nM/P2Y2, 400 nM/P2Y4, 20 μM/P2Y6, >100 μM/P2Y1 by calcium mobilization using respective 1321N P2Y subtype transfectants). In addition to its in vivo efficacy in anmial dry eye models, diquafosol is also shown to enhance mucociliary clearance in sheep and stimulate vaginal moisture in ovariectomized rabbits.
P2Y2/P2Y4 purinoceptor agonist: EC50 = 0.10 μM at P2Y2, 0.4 μM at P2Y4 (20 μM at P2Y6) in 1321N astrocytoma cells infected with a retrovirus encoding the human P2Y1, P2Y2, P2Y4 and P2Y6
Diagnostic Implications
In clinical development for the treatment of dry eye and chronic lung disease, such as cystic fibrosis
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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