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Daurisoline
| Product Name | Daurisoline |
| Price: | $108 / 20mg |
| Catalog No.: | CN01211 |
| CAS No.: | 70553-76-3 |
| Molecular Formula: | C37H42N2O6 |
| Molecular Weight: | 610.73 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | The roots of Menispermum dauricum |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | COc1cc2c(cc1OC)CCN([C@@H]2Cc1ccc(cc1)Oc1cc(ccc1O)C[C@H]1N(C)CCc2c1cc(O)c(c2)OC)C |
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| Description | Daurisoline is a hERG inhibitor and also an autophagy blocker. |
| Target | hERG[1], autophagy[2] |
| In Vitro | Daurisoline (compound 1) shows a maximal inhibitory effect on the end of depolarization (IhERG-step) at +20 mV and on the peak tail current (IhERG-tail) at +60 mV. At concentrations of 1, 3, 10, and 30 μM, the inhibition ratios for current amplitude at the end of depolarization (IhERG-step) are 32.2±4.2%, 41.6±2.6%, 62.1±5.9%, and 74.8±6.8%, respectively; the IC50 is 9.1 μM. In turn, the inhibition ratios for IhERG-tail are 16.7±5.8%, 31.1±4.5%, 55.1±7.2%, and 81.2±7.0%, respectively; the IC50 is 9.6 μM[1]. Daurisoline (DAS) inhibits the CPT-induced autophagy in different cancer cell lines, with IC50s of 74.75±1.03, 50.54±1.02 and 80.81±1.10 μM in HeLa, A549 and HCT-116 cells, respectively. DAC and Daurisoline also impair lysosomal function and lysosomal acidification, via inhibiting the lysosome V-type ATPase acitivity in DAC and Daurisoline treated cells[2]. |
| In Vivo | The results show that plasma concentration exists a biexponential decline following iv administration of Daurisoline (DS) or dauricine (Dau) 6 mg/kg. After iv Daurisoline and Dau 6 mg/kg in beagle dogs, HR, LVSP, dp/dtmax, and SBP are decreased. But the maximum pharmacological effects of both drugs peak at 10 to15 min later than the maximum plasma concentration is observed[3]. |
| Cell Assay | Cell proliferation is determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. HeLa cells are seeded at 7000 cells per well in 96-well plates in DMEM (1% serum). After cells are treated with different compounds (including Daurisoline) for indicated times, 20 μL of MTT (2.5 mg/mL in PBS) is added to each well. The plates are incubated for an additional 4 h at 37°C. Then the purple-blue MTT formazan precipitate is dissolved in 100 μL DMSO. The cell viability of HeLa cell is evaluated by measuring optical density at 572 nm with a microplate reader[2]. |
| Animal Admin | After the beagle dogs are anesthetized with sodium pentobarbital (30 mg/kg, iv) a canula is advanced into the left ventricle through the right common carotid artery. And the canula is connected to a pressure transducer which is connected to an amplifier and polygraph. The right femoral artery is canulated to measure the blood pressure wave. ECG (lead II) is observed simultaneously. After iv injection of Daurisoline (DS) (n=4) or Dau (n=4) to beagle dogs, the ECG, BP, and LVP signals are recorded. Blood samples are taken before dosing and at 2, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 6, 8 h after dosing[3]. |
| Density | 1.2±0.1 g/cm3 |
| Boiling Point | 724.5±60.0 °C at 760 mmHg |
| Flash Point | 392.0±32.9 °C |
| Exact Mass | 610.304260 |
| PSA | 83.86000 |
| LogP | 5.84 |
| Vapour Pressure | 0.0±2.4 mmHg at 25°C |
| Storage condition | ?20°C |