α-Hydroxyglutaric acid (2-Hydroxyglutarate) is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases.
| Molecular Weight | 148.11 |
| Formula | C5H8O5 |
| CAS Number | 2889-31-8 |
| Form | Liquid |
| Storage | -20°C |
| 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.
[1] James A Nathan. Science. Metabolite-driven antitumor immunity
[2] Yi-Ping Wang, et al. J Biol Chem. Metabolite sensing and signaling in cancer
[3] Petr Ježek. Antioxid Redox Signal. 2-Hydroxyglutarate in Cancer Cells
[4] Takeo Fujii, et al. Discov Med. Targeting isocitrate dehydrogenase (IDH) in cancer
[5] Lenny Dang, et al. Nature. Cancer-associated IDH1 mutations produce 2-hydroxyglutarate
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