Synonym: 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
CAS Number: 211427-08-6
Empirical Formula (Hill Notation): C18H22N4Na4O23P4
Molecular Weight: 878.23
Linear Formula: C18H22N4Na4O23P4
Product Type: Chemical
| assay |
>95% (HPLC) |
| color |
white to beige |
| form |
powder |
| optical activity |
[α]/D -12.0 to -8.0°, c = 1.0 in H2O |
| Quality Level |
100  |
| solubility |
H2O: 2 mg/mL, clear |
| storage temp. |
−20°C |
| 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. |
| Biochem/physiol Actions: |
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 Germany |
WGK 3 |
| Flash Point(F) |
Not applicable |
| Flash Point(C) |
Not applicable |
| Purity |
>95% (HPLC) |
| Storage Temp. |
−20°C |
| UNSPSC |
12352200 |
