化学信息：
| 中文名 | 蝙蝠葛苏林碱 |
| 英文名 | Daurisoline |
| 中文别名 | - |
| 英文别名 | (R,R)-Daurisoline |
| 来源 | 蝙蝠葛Menispermum dauricum DC. |
| 化合物类型 | 生物碱(Alkaloids)>异喹啉生物碱>双苄基异喹啉生物碱 |
| 化学式 | C37H42N2O6 |
| 分子量 | 610.74 |
| CAS号 | 70553-76-3 |
| 纯度 | 98%, HPLC |
| 溶剂/溶解度 | DMSO: 50 mg/ml (81.87 mM); Water : < 0.1 mg/ml (insoluble) |
| 溶液配制 | 10mg加入1.64ml DMSO，或者每6.11mg加入1ml DMSO，配制成10mM溶液。 |
生物信息
| 产品描述 | Daurisoline is a hERG inhibitor and also an autophagy blocker. | ||||
| 信号通路 | Autophagy | ||||
| 靶点 | hERG | - | - | - | - |
| IC50 | 9.1 μM | - | - | - | - |
| 体外研究 | Daurisoline 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. 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. | ||||
| 体内研究 | 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. | ||||
| 临床实验 | N/A | ||||
1. Liu Q, et al. J Nat Prod. 2012,75(9):1539-45.
2. Wu MY, et al. Oncotarget. 2017,8(44):77673-77684.
3. Shi SJ, et al. Acta Pharmacol Sin. 2003,24(10):1011-5.
包装清单：| 产品编号 | 产品名称 | 包装 |
| SM4112-10mM | 蝙蝠葛苏林碱(98%, HPLC) | 10mM×0.2ml |
| SM4112-5mg | 蝙蝠葛苏林碱(98%, HPLC) | 5mg |
| SM4112-25mg | 蝙蝠葛苏林碱(98%, HPLC) | 25mg |
| - | 说明书 | 1份 |
-20℃保存，至少一年有效。固体粉末4℃保存，至少一个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
注意事项：本产品可能对人体有一定的毒害作用，请注意适当防护，以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
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