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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 |
[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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