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L-2-Hydroxyglutaric acid disodium ((S)-2-Hydroxyglutaric acid disodium, L-2-Hydroxyglutarate disodium, LGA, L-2HG) is an epigenetic modifier and a putative oncometabolite in kidney cancer that inhibits histone demethylases and hence promotes histone methylation. L-2-Hydroxyglutaric acid disodium is also an inhibitor of mitochondrial creatine kinase (Mi-CK) with Km and Ki of 2.52 mM and 11.13 mM, respectively.
| Molecular Weight | 192.08 |
| Formula | C5H6Na2O5 |
| CAS Number | 63512-50-5 |
| Solubility (25°C) | Water 38 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.
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TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC50 of 2.9 nM. It is an orally administered CNS-permeable clinical candidate for the study of neurodevelopmental disorders, such as autism spectrum disorders. |
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