Chst15-IN-1 is a potent reversible covalent Chst15 inhibitor. Chst15-IN-1 effectively inhibits chondroitin sulfate-E (CS-E) sulfation levels and other closely related glycosaminoglycans (GAG) sulfotransferases. Chst15-IN-1, as a selective sulfotransferase inhibitor, can diminish the inhibitory effects of chondroitin sulfate proteoglycans (CSPGs), and can be used for the stimulation of neuronal repair[1].
Chst15-IN-1 (25 μM; 24 hours; Neu7 astrocytes) is selective for sulfotransferases over the myriad of reactive cysteine-containing proteins. Chst15-IN-1 (10 and 25 μM; Neu7 astrocytes) shows a significant dose dependent decrease in cell-surface CS-E expression[1].
Chst15-IN-1 (3.0 mg/kg; i.v.) has a moderate clearance of 21 mL/min/kg, moderate volume of distribution of 0.97 L/kg, and short terminal half-life of 1.6 hours[1].
| Animal Model: | Rats |
| Dosage: | 3.0 mg/kg (Pharmacokinetic Analysis) |
| Administration: | I.v. |
| Result: | Had a moderate clearance of 21 mL/min/kg, moderate volume of distribution of 0.97 L/kg, and short terminal half-life of 1.6 h. |