Imirestat (AL 1576) is an aldose reductase inhibitor, used for the treatment of diabetes.
| Molecular Weight | 286.23 |
| Formula | C15H8F2N2O2 |
| CAS Number | 89391-50-4 |
| Form | Solid |
| Solubility (25°C) | DMSO 83.33 mg/mL (ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
[5] J Y Chien, et al. Pharm Res. Saturable tissue binding and imirestat pharmacokinetics in rats
| Related Aldose Reductase Products |
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AKR1C3-IN-10 is a selective AKR1C3 inhibitor (IC50=51 nM). |
| Dehydroglyasperin D
Dehydroglyasperin D inhibits rat and human Aldose Reductase (AR) (IC50: 62.4 μM and 176.2 μM respectively). |
| Ganoderic acid Df
Ganoderic acid Df is a lanostane-type triterpenoid, that can be isolated from the fruiting body of Ganoderma lucidum. |
| Danshenol A
Danshenol A is an aldose reductase (AR) inhibitor with an IC50 of 0.1 μM. Danshenol A can protect endothelial cells from oxidative stress by directly scavenging ROS. Danshenol A has anti-inflammatory and antitumor properties. |
| Hydroxyevodiamine
Hydroxyevodiamine (Rhetsinine) inhibits aldose reductase with an IC50 value of 24.1 μM. |
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