Daurisoline (Synonyms: 蝙蝠葛苏林碱; (R,R)-Daurisoline) 纯度: 99.65%
Daurisoline 是一个 hERG 抑制剂,也是一种自噬抑制剂。
Daurisoline Chemical Structure
CAS No. : 70553-76-3
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥1035 | In-stock | |
5 mg | ¥770 | In-stock | |
10 mg | ¥1350 | In-stock | |
25 mg | ¥2850 | In-stock | |
50 mg | ¥5200 | In-stock | |
100 mg | 询价 | ||
200 mg | 询价 |
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Daurisoline 相关产品
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生物活性 |
Daurisoline is a hERG inhibitor and also an autophagy blocker. |
IC50 & Target |
hERG[1], autophagy[2] |
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体外研究 (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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
610.74 |
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Formula |
C37H42N2O6 |
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CAS 号 |
70553-76-3 |
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中文名称 |
蝙蝠葛苏林碱 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 100 mg/mL (163.74 mM; Need ultrasonic) 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Kinase Assay [2] |
HEK293 cells are incubated overnight with 35 μg/mL Dx-OG514. Cells are washed and incubated with serum-free Dulbecco’s modified Eagle’s medium (DMEM) for 2 h. 15 minutes prior to lysis, FCCP is added into the medium to a final concentration of 1 μM. Cells are scraped in fraction buffer (50 mM KCl, 90 mM K-Gluconate, 1 mM EGTA, 50 mM Glucose, 20 mM HEPES, protease inhibitor cocktail, pH=7.4) supplemented with 1 μM FCCP. After spraying with needle, cells are spun down at 10,000 rpm for 15 sec. at 4°C. Then, re-centrifuge the supernatant at max speed for another 20 minutes. The pellet is resuspended in pre-warmed fractionation buffer supplemented with 1% BSA, and split into several aliquots with DAC, Daurisoline (DAS) or BAF treatment for 30 min. Baseline fluorescence is measured at 530 nm upon 511 nm excitation in 96-well plate at 30 s intervals for 5 min[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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Cell Assay [2] |
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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
Animal Administration [3] |
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]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
参考文献 |
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