Biochem/physiol Actions
Draflazine (R88021; (-)-R75231), is a potent nucleoside transporter ENT1 (SLC29A1) inhibitor with 370-fold selectivity over ENT2 (SLC29A2). R88021 exhibits 30- and 40-times higher affinity as (+)-R75231 (R88016) using calf lung membrane preparation (by [3H]R75231 & [3H]NBI displacement) and intact human erythrocytes (by [3H]NBMPR displacement), respectively. Draflazine is 20-times more potent as R88016 in enhancing adenosine potency against ADP-induced aggregation in human whole blood (IC50 = 0.5 μM vs 10 μM with 1 μM respective inhibitor), Draflazine and R75231, but not R88016, show cardioprotective efficacy against catecholamines infusion in rabbits in vivo.
Potent nucleoside transporter ENT1 (SLC29A1) inhibitor with 370-fold selectivity over ENT2 (SLC29A2) and cardioprotective efficacy in vivo.
| assay | ≥98% (HPLC) |
| form | powder |
| optical activity | [α]/D -23 to -29°, c = 0.5 in ethanol |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | room temp |
| SMILES string | Fc1ccc(cc1)C(CCCCN3CC(N(CC3)CC(=O)Nc4c(cc(cc4Cl)N)Cl)C(=O)N)c2ccc(cc2)F |
| InChI | 1S/C30H33Cl2F2N5O2/c31-25-15-23(35)16-26(32)29(25)37-28(40)18-39-14-13-38(17-27(39)30(36)41)12-2-1-3-24(19-4-8-21(33)9-5-19)20-6-10-22(34)11-7-20/h4-11,15-16,24,27H,1-3,12-14,17-18,35H2,(H2,36,41)(H,37,40) |
| InChI key | IWMYIWLIESDFRZ-UHFFFAOYSA-N |
