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Tautomycetin is a potent and specifical PP1 inhibitor with the potential apoptosis-inducing activity. Tautomycetin inhibits purified PP1 and PP2A enzymes with IC50s of 1.6 nM and 62 nM, respectively.
Tautomycetin is an antifungal antibiotic and has immunosuppressive effects in vivo. Tautomycetin (intraperitoneal injection; 0.03 mg/kg-5 mg/kg; 30 days) exhibits in vivo immunosuppressive effect in in vivo heart allograft transplantation. And the biochemical analysis of GOP, GTP, glucose, and creatine levels in blood after administration of TMC up to 5 mg/kg in rats for 30 days does not show any significant liver and kidney toxicity in rats.
| Molecular Weight | 606.74 |
| Formula | C33H50O10 |
| CAS Number | 119757-73-2 |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage | -20°C, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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