Lithocholic acid is a toxic secondary bile acid, causes intrahepatic cholestasis, has tumor-promoting activity, its toxic effect can be protected after it activates the vitamin D receptor, PXR and FXR. Lithocholic acid directly binds VDR (vitamin D receptor) with Ki of 29μM, activates VDR (vitamin D receptor) 30 μM, with much more sensitivity than the other nuclear receptors (eg. PXR, FXR), and its toxic effect is thus protected. Lithocholic acid has tumor-promoting activity, inhibits mammalian DNA Polymerase β with IC50 of 15 μM.
| Molecular Weight | 376.57 |
| Formula | C24H40O3 |
| CAS Number | 434-13-9 |
| Solubility (25°C) | DMSO > 100 mg/mL Ethanol 10 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.
[2] Sunil Gaikwad, et al. Lithocholic acid-based design of noncalcemic vitamin D receptor agonists
[3] Harue Sasaki, et al. Lithocholic Acid Derivatives as Potent Vitamin D Receptor Agonists
[4] Sonja Sivcev, et al. Lithocholic acid inhibits P2X2 and potentiates P2X4 receptor channel gating
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