SML3058

Diquafosol tetrasodium

>95% (HPLC)

• Sinônimo(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
• Fórmula empírica (Notação de Hill): C₁₈H₂₂N₄Na₄O₂₃P₄
• Número CAS: 211427-08-6
• Peso molecular: 878.23
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: >95% (HPLC)
• Formulário: powder
• atividade óptica: [α]/D -12.0 to -8.0°, c = 1.0 in H₂O
• cor: white to beige
• solubilidade: H₂O: 2 mg/mL, clear
• temperatura de armazenamento: −20°C
• cadeia de caracteres SMILES: [Na].[Na].[Na].[Na].[P](=O)(O[P](=O)(O[P](=O)(OC[C@H]3O[C@H]([C@@H]([C@@H]3O)O)N4C=CC(=O)NC4=O)O)O)(O[P](=O)(OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)N2C=CC(=O)NC2=O)O)O
• InChI: 1S/C18H26N4O23P4.4Na/c23-9-1-3-21(17(29)19-9)15-13(27)11(25)7(41-15)5-39-46(31,32)43-48(35,36)45-49(37,38)44-47(33,34)40-6-8-12(26)14(28)16(42-8)22-4-2-10(24)20-18(22)30;;;;/h1-4,7-8,11-16,25-28H,5-6H2,(H,31,32)(H,33,34)(H,35,36)(H,37,38)(H,19,23,29)(H,20
• chave InChI: MHPMESDJCUICEY-FNXFGIETSA-N

Descrição

Ações bioquímicas/fisiológicas

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 P2Y_1, P2Y_2, P2Y₄ and P2Y₆

Implicações do diagnóstico

In clinical development for the treatment of dry eye and chronic lung disease, such as cystic fibrosis

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable