产品说明书
Tanshinone IIA sulfonate sodium
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同义名 : | 丹参酮IIA磺酸盐 ;Sodium Tanshinone IIA sulfonate;Tanshinone IIA sodium sulfonate;DS-201;Danshen-201;Tanshinone II A sulfonate;TIIAS;Sulfotanshinone sodium II-A;Tanshinone IIA sulfonate (sodium salt) |
| CAS号 : | 69659-80-9 | |
| 货号 : | A255311 | |
| 分子式 : | C19H17NaO6S | |
| 纯度 : | 98% | |
| 分子量 : | 396.389 | |
| MDL号 : | MFCD09028094 | |
| 存储条件： |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 60 mg/mL(151.37 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 2 mg/mL(5.05 mM)，配合低频超声，并水浴加热至45℃助溶 |
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| 动物实验配方： |
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| 描述 | Tanshinone IIA Sulfonate Sodium (STS) is a derivative of tanshinone IIA, which acts as an inhibitor of store-operated Ca2+ entry (SOCE), and is used to treat cardiovascular disorders. Morris water maze results showed that oral administration of STS (10 mg/kg and 20 mg/kg) and Donepezil shortened escape latency, increased crossing times of the original position of the platform, and increased the time spent in the target quadrant. STS decreased the activity of acetylcholinesterase (AChE) and increased the activity of choline acetyltransferase (ChAT) in the hippocampus and cortex of SCOP-treated mice[3]. Sodium Tanshinone IIA sulfonate (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats[4]. Sodium tanshinone IIA sulfonate inhibits the activity of CYP3A4 in a dose-dependent manner by the HLMs and CYP3A4 isoform. The KM and Vmax values of STS are 54.8±14.6 µM and 0.9±0.1 nmol/mg protein/min, respectively, for the HLMs and 7.5±1.4 µM and 6.8±0.3 nmol/nmol P450/min, respectively, for CYP3A4. CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP2E1, and CYP2C19 show minimal or no effects on the metabolism of STS[5]. STS significantly ameliorated pulmonary inflammatory responses, mucus hypersecretion and lung function decline in CS-exposed mice challenged with LPS. STS treatment also significantly attenuated increased IL-6 and IL-8 releases from cigarette smoke extract (CSE)-treated human bronchial epithelial cells (16HBE) challenged with LPS[6]. Intermittent hypoxia treatment resulted in high oxidative stress and low apoptosis in Lewis lung carcinoma-implanted mice, which could be attenuated by sodium tanshinone IIA sulfonate administration possibly through a mechanism mediated by the nuclear factor erythroid 2-related factor 2/nuclear factor kappa B signaling pathway[7]. | ||
| 临床研究 | |||||
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| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02524964 | Left Ventricular Remodeling ... 展开 >> Acute Myocardial Infarction 收起 << | Phase 4 | Unknown | July 2017 | China, Guangdong ... 展开 >> Guangdong Provincial Hospital of Chinese Medicine Recruiting Guangzhou, Guangdong, China, 510120 Contact: Minzhou Zhang, Dr. 86-20-81887233 ext 32801 minzhouzhang@yeah.net Contact: Liheng Guo, Dr. 86-8187236 ext 32907 lihengguo1@yeah.net 收起 << |
| NCT01637675 | Pulmonary Hypertension ... 展开 >> Pulmonary Arterial Hypertension Cardiovascular Diseases Lung Diseases Tanshinone IIA Sulfonate 收起 << | Phase 2 Phase 3 | Unknown | December 2014 | China, Guangdong ... 展开 >> The First Affiliated Hospital of Guangzhou Medical University Recruiting Guangzhou, Guangdong, China, 510120 Contact: Jian Wang, MD +8615013388183 jwang31@jhmi.edu 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.52mL 0.50mL 0.25mL |
12.61mL 2.52mL 1.26mL |
25.23mL 5.05mL 2.52mL |
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