DRAFLAZINE
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.
| Colour | white to beige |
|---|---|
| InChI key | IWMYIWLIESDFRZ-UHFFFAOYSA-N |
| 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/h4-11,15-16,2 |
| Manufacturer | SIGMA-ALDRICH |
| Storage Temp. | room temp |
| Solubility | DMSO: 2 mg/mL, clear |
| Form | powder |
| Assay | ≥98% (HPLC) |
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