| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
Daurisoline (compound 1) demonstrated greatest inhibitory effects on the depolarization endpoint (IhERG-step) at +20 mV and the peak tail current (IhERG-tail) at +60 mV. The inhibition rates of current amplitude at the conclusion of depolarization (IhERG step) were 32.2±4.2%, 41.6±2.6%, 62.1±5.9% and 74.8±6.8% at doses of 1, 3, 10 and 30 μM, respectively; IC50 = 9.1 μM. In turn, the inhibition rates of IhERG-tail were 16.7±5.8%, 31.1±4.5%, 55.1±7.2% and 81.2±7.0% correspondingly; the IC50 was 9.6 μM[1]. Daurisoline (DAS) suppresses CPT-induced autophagy in distinct cancer cell lines, with IC50 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 both impair lysosomal function and lysosomal acidification by suppressing lysosomal V-type ATPase activity in DAC- and Daurisoline-treated cells [2].
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| ln Vivo |
The findings demonstrated that a bi-exponential drop in plasma concentrations occurred following an intravenous injection of either daucine (Dau) or dausoline (DS) at a dose of 6 mg/kg. After beagle dogs received intravenous daurisoline and dau (6 mg/kg), there was a decrease in HR, LVSP, dp/dtmax, and SBP. But both medications' maximal pharmacological effects peak 10 to 15 minutes after their highest blood concentration [3].
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| References |
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| Additional Infomation |
Daurisoline is a member of isoquinolines.
Daurisoline has been reported in Menispermum dauricum with data available. |
| Molecular Formula |
C37H42N2O6
|
|---|---|
| Molecular Weight |
610.7392
|
| Exact Mass |
610.304
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| CAS # |
70553-76-3
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| PubChem CID |
51106
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
724.5±60.0 °C at 760 mmHg
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| Melting Point |
96-102ºC
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| Flash Point |
392.0±32.9 °C
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| Vapour Pressure |
0.0±2.4 mmHg at 25°C
|
| Index of Refraction |
1.618
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| LogP |
5.84
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
9
|
| Heavy Atom Count |
45
|
| Complexity |
917
|
| Defined Atom Stereocenter Count |
2
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| SMILES |
CN1CCC2=CC(=C(C=C2[C@H]1CC3=CC=C(C=C3)OC4=C(C=CC(=C4)C[C@@H]5C6=CC(=C(C=C6CCN5C)OC)O)O)OC)OC
|
| InChi Key |
BURJAQFYNVMZDV-FIRIVFDPSA-N
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| InChi Code |
InChI=1S/C37H42N2O6/c1-38-15-13-26-20-36(43-4)37(44-5)22-29(26)30(38)16-23-6-9-27(10-7-23)45-35-18-24(8-11-32(35)40)17-31-28-21-33(41)34(42-3)19-25(28)12-14-39(31)2/h6-11,18-22,30-31,40-41H,12-17H2,1-5H3/t30-,31-/m1/s1
|
| Chemical Name |
(1R)-1-[[3-[4-[[(1R)-6,7-dimethoxy-2-methyl-3,4-dihydro-1H-isoquinolin-1-yl]methyl]phenoxy]-4-hydroxyphenyl]methyl]-6-methoxy-2-methyl-3,4-dihydro-1H-isoquinolin-7-ol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~163.74 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 20 mg/mL (32.75 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6374 mL | 8.1868 mL | 16.3736 mL | |
| 5 mM | 0.3275 mL | 1.6374 mL | 3.2747 mL | |
| 10 mM | 0.1637 mL | 0.8187 mL | 1.6374 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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