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69659-80-9

中文名称 丹参酮IIA-磺酸钠
英文名称 TanshinoneIIA
CAS 69659-80-9
分子式 C19H19NaO6S
分子量 398.4
MOL 文件 69659-80-9.mol
更新日期 2024/05/22 10:39:06
69659-80-9 结构式 69659-80-9 结构式

基本信息

中文别名
丹参酮IIA磺酸盐
丹参酮IIA-磺酸钠(标准品)
TANSHINONE IIA-SULFONIC SODIUM 丹参酮IIA-磺酸钠
英文别名
DS 201
Sodium 1,6,6-trimeth
Sodium TanshinonⅡA SilateA
Sodium Tanshinon Ⅱ Asilate
Sulfotanshinone sodiuM II-A
Tanshinone ⅡA-sulfonic sodium
Tanshinone ⅡASulfonate SodiuM
SodiuM tanshinone IIA sulfonate
Sulfotanshinone SodiuM Injection
Tanshinone IIA sulfonate (sodium)

物理化学性质

外观性状红色结晶粉末,可溶于甲醇、乙醇、DMSO等有机溶剂,来源于丹参根茎。
熔点To dark to Visualize
储存条件Inert atmosphere,2-8°C
溶解度可溶于DMSO(少许)、甲醇(少许)
形态固体
颜色红色

应用领域

用途1
一种p2x7的有效负性变构调节剂。
用途2
丹参酮IIA磺酸钠可用于冠心病、心绞痛、心肌梗死,也可用于室性早搏,用于胸肋胁痛,风湿痹痛,症瘕结块,疮疡肿痛,跌扑伤痛,月经不调,闭经痛经,产后淤痛等。

常见问题列表

生物活性
Tanshinone IIA sulfonate sodium 是 tanshinone IIA 的衍生物,为 SOCE 的抑制剂,用于心血管疾病的研究。
靶点
TargetValue
SOCE
()
P2X7
()
CYP3A4
(Cell-free assay)
6.377 μM
体外研究

Sodium Tanshinone IIA sulfonate (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats. The suppressive effects of Sodium Tanshinone IIA sulfonate on TRPC1 and TRPC6 expression in hypoxic PASMCs can be prevented by specific knockdown PKG or PPAR-γ. The suppressive effects of Sodium Tanshinone IIA sulfonate on basal calcium concentration and SOCE in hypoxic PASMCs can be reversed by specific knockdown of PKG or PPAR-γ. PKG-PPAR-γ signaling axis participates in the suppressive effects of Sodium Tanshinone IIA sulfonate on proliferation in hypoxic PASMCs. PPAR-γ agonist promotes the protective role of Sodium Tanshinone IIA sulfonate on basal [Ca 2+ ]i and SOCE in hypoxic PASMCs. Sodium tanshinone IIA sulfonate inhibits the activity of CYP3A4 in a dose-dependent manner by the HLMs and CYP3A4 isoform. The K M 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. Sodium Tanshinone IIA sulfonate inhibits the activity of CYP3A4 in a dose-dependent manner in the HLMs and CYP3A4 isoform. Sodium Tanshinone IIA sulfonate primarily inhibits the activities of CYP3A4 in vitro, and Sodium Tanshinone IIA sulfonate has the potential to perpetrate drug-drug interactions with other CYP3A4 substrates.

体内研究

Sodium Tanshinone IIA sulfonate (10 mg/kg, 20 mg/kg) and Donepezil shorten escape latency, increase crossing times of the original position of the platform, and increase the time spent in the target quadrant. Sodium Tanshinone IIA sulfonate decreases the activity of acetylcholinesterase (AChE) and increases the activity of choline acetyltransferase (ChAT) in the hippocampus and cortex of SCOP-treated mice. Sodium Tanshinone IIA sulfonate increases the activity of superoxide dismutase (SOD) and decreases the levels of malondialdehyde (MDA) and reactive oxygen species (ROS) in hippocampus and cortex. Sodium Tanshinone IIA sulfonate prevention (30 mg/kg/day) alleviates hypoxia-induced characteristic changes in chronic hypoxia PH rat model. Sodium Tanshinone IIA sulfonate (20, 10, and 5 mg/kg, i.p.) effectively prevents peritoneal adhesion without affecting anastomotic healing in the rats. Compared with the adhesion model group, the Sodium Tanshinone IIA sulfonate-treated groups show increased peritoneal lavage fluid tPA activity and tPA/PAI-1 ratio in the ischemic tissues with loared TGF-β1 and collagen I expressions in the ischemic tissues.

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