SML3058

Diquafosol tetrasodium

>95% (HPLC)

• 別名: 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
• 実験式（ヒル表記法）: C₁₈H₂₂N₄Na₄O₂₃P₄
• CAS番号: 211427-08-6
• 分子量: 878.23
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: >95% (HPLC)
• フォーム: powder
• 光学活性: [α]/D -12.0 to -8.0°, c = 1.0 in H₂O
• 色: white to beige
• 溶解性: H₂O: 2 mg/mL, clear
• 保管温度: −20°C
• SMILES記法: [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
• InChI Key: MHPMESDJCUICEY-FNXFGIETSA-N

詳細

生物化学的／生理学的作用

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

診断上の意義

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable