Ponalrestat is an orally active, selective and noncompetitive aldose reductase inhibitor. Ponalrestat selectively inhibits ALR2 (Ki=7.7 nM) over ALR1 (Ki=60 μM). Ponalrestat activates lipoprotein lipase (LPL) activity in the adipose tissue and alleviates the cachectic symptoms induced by B16 melanoma in mice. Ponalrestat is effective in the attenuation of the cachectic symptoms induced by human melanomas G361 and SEKI in nude mice.
| Molecular Weight | 391.19 |
| Formula | C17H12BrFN2O3 |
| CAS Number | 72702-95-5 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 50 mg/mL |
| 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.
| Related Aldose Reductase Products |
|---|
| AKR1C3-IN-10
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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