Tanshinone IIA sulfonate sodium

For research use only. Not for use in humans.

目录号:S3766 中文名称:丹参酮IIA-磺酸钠

Tanshinone IIA sulfonate sodium Chemical Structure

CAS No. 69659-80-9

Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC).

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产品安全说明书

P450 (e.g. CYP17)抑制剂选择性比较

生物活性

产品描述 Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen. Sodium tanshinone IIA sulfonate (STS) is a potent negative allosteric modulator of the human purinergic receptor P2X7. Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 and store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC).
靶点
SOCE [2]
()
P2X7 [4]
()
CYP3A4 [1]
(Cell-free assay)
6.377 μM
体外研究

Sodium tanshinone IIA sulfonate (STS) inhibits the activity of CYP3A4 in a dose-dependent manner in the HLMs and CYP3A4 isoform. Other CYP isoforms, including CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP2E1, and CYP2C19, show minimal or no effect on the metabolism of STS. Thus, STS is a potent inhibitor for CYP3A4[1]. STS upregulates the protein expression of Bcl-2 and downregulates the proteins expression of Bax and Caspase-3[2]. Sodium tanshinone IIA sulfonate (STS) inhibits store-operated Ca2+ entry (SOCE) through store-operated Ca2+ channels (SOCC) via downregulating the expression of transient receptor potential canonical proteins (TRPC). STS treatment can effectively prevent the hypoxia-mediated inhibition of the PKG-PPAR-γ signaling axis in rat distal pulmonary arterial smooth muscle cells (PASMCs) and distal pulmonary arteries. It can also prevent hypoxia-mediated increases in intracellular calcium homeostasis and cell proliferation, by targeting and restoring the hypoxia-inhibited PKG-PPAR-γ signaling pathway in PASMCs[3].

体内研究

The metabolic rate of Sodium tanshinone IIA sulfonate (STS) in rats is fast, the T1/2 is not more than 0.9 h[1]. tanshinone IIA has been reported to possess neuroprotective effects against Alzheimer’s disease (AD). STS decreases the activity of acetylcholinesterase (AChE) and increases the activity of choline acetyltransferase (ChAT) in the hippocampus and cortex of SCOP-treated mice. It increases the activity of superoxide dismutase (SOD) and decreases the levels of malondialdehyde (MDA) and reactive oxygen species (ROS) in hippocampus and cortex. STS administration (10 mg/kg and 20 mg/kg) could improve SCOP-induced learning and memory impairment in Kunming mice. Meanwhile, STS could obviously improve central cholinergic neurotransmission and attenuate oxidative damage. STS has cardioprotective effects on cardiovascular injury[2]. STS has been clinically used for decades in the treatment of numerous cardiovascular diseases, such as hypertension, atherosclerosis, and others[3].

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[3]

- 合并
  • Cell lines: pulmonary arterial smooth muscle cells (PASMCs)
  • Concentrations: 12.5 μM
  • Incubation Time: 60 h
  • Method:

    Rat PASMCs are digested by collagenase and then cultured in low-sugar DMEM medium containing 10% fetal bovine serum. When the fusion of cells is at 60-70%, the medium is replaced with the low-sugar DMEM medium containing 0.5% fetal bovine serum in which cells are cultured for 24 h to be homogenized. After the cells are grown to ∼80%, they are randomly divided into four groups, two of which are treated with STS (12.5 μM). STS group and STS-free group are randomly exposed to normoxic environment and hypoxic conditions (4% O2, 60 h). 60 h of prolonged hypoxic stress (4% O2) can effectively lead to elevated proliferation and migration of primary cultured distal PASMCs. This mimics similar hypoxic responses as the PASMCs isolated from the CHPH rats, as the hypoxic elevation of [Ca2+]i, SOCE, and upregulation of TRPC expression in cultured PASMCs only occur at 60 h or later time points of hypoxic exposure. In this study, both incubators are set to 37°C, 5% CO2. The total protein of these cells is extracted by RIPA buffer.


    (Only for Reference)
动物实验:

[2]

- 合并
  • Animal Models: Kunming mice
  • Dosages: 10 mg/kg and 20 mg/kg
  • Administration: oral administration
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 79 mg/mL (199.29 mM)

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 396.39
化学式

C19H17O6S.Na

CAS号 69659-80-9
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
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% DMSO % % Tween 80 % ddH2O
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    V1
    C2
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    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID