生物活性分子抑制剂Tanshinone IIA sulfonate sodium(Synonyms: 丹参酮IIA磺酸盐; Sodium Tanshinone IIA sulfonate; Tanshinone IIA sodium sulfonate)

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Tanshinone IIA sulfonate sodium (Synonyms: 丹参酮IIA磺酸盐; Sodium Tanshinone IIA sulfonate; Tanshinone IIA sodium sulfonate) 纯度: ≥98.0%

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。

Tanshinone IIA sulfonate sodium(Synonyms: 丹参酮IIA磺酸盐; Sodium Tanshinone IIA sulfonate;  Tanshinone IIA sodium sulfonate)

Tanshinone IIA sulfonate sodium Chemical Structure

CAS No. : 69659-80-9

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生物活性

Tanshinone IIA sulfonate (sodium) is a derivative of tanshinone IIA, which acts as an inhibitor of store-operated Ca2+ entry (SOCE), and is used to treat cardiovascular disorders.

体外研究
(In Vitro)

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 [Ca2+]i and SOCE in hypoxic PASMCs[2]. 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[3]. 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[4].

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.

体内研究
(In Vivo)

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[1]. Sodium Tanshinone IIA sulfonate prevention (30 mg/kg/day) alleviates hypoxia-induced characteristic changes in chronic hypoxia PH rat model[2]. 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[5].

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.

Clinical Trial

分子量

396.39

Formula

C19H17NaO6S

CAS 号

69659-80-9

中文名称

丹参酮IIA磺酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*该产品在溶液状态不稳定,建议您现用现配,即刻使用。

溶解性数据
In Vitro: 

DMSO : 62.5 mg/mL (157.67 mM; Need ultrasonic)

H2O : 8.33 mg/mL (21.01 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5228 mL 12.6138 mL 25.2277 mL
5 mM 0.5046 mL 2.5228 mL 5.0455 mL
10 mM 0.2523 mL 1.2614 mL 2.5228 mL

*

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;该产品在溶液状态不稳定,建议您现用现配,即刻使用

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
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.25 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.25 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: 2.08 mg/mL (5.25 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (5.25 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Xu QQ, et al. Sodium Tanshinone IIA Sulfonate Attenuates Scopolamine-Induced Cognitive Dysfunctions via Improving Cholinergic System. Biomed Res Int. 2016;2016:9852536

    [2]. Jiang Q, et al. Sodium tanshinone IIA sulfonate inhibits hypoxia-induced enhancement of SOCE in pulmonary arterial smooth muscle cells via the PKG-PPAR-γ signaling axis. Am J Physiol Cell Physiol. 2016 Jul 1;311(1):C136-49.

    [3]. Ouyang DS, et al. Kinetics of cytochrome P450 enzymes for metabolism of sodium tanshinone IIA sulfonate in vitro. Chin Med. 2016 Mar 22;11:11.

    [4]. Chen D, et al. Sodium tanshinone IIA sulfonate and its interactions with human CYP450s. Xenobiotica. 2016 Dec;46(12):1085-1092. Epub 2016 Mar 2.

    [5]. Lin S, et al. [Sodium tanshinone IIA sulfonate prevents postoperative peritoneal adhesions in rats by enhancing the activity of the peritoneal fibrinolytic system]. Nan Fang Yi Ke Da Xue Xue Bao. 2016 Feb;36(2):260-4.

Animal Administration
[1][2]

Mice[1]
Male Kunming mice (KM, weighing 35-40 g) are maintained on standard laboratory conditions with free access to water and food. Mice are randomly divided into five groups: vehicle control group (CON, 0.9% saline, n=10), scopolamine group (SCOP, n=10), low dose Sodium Tanshinone IIA sulfonate group (Sodium Tanshinone IIA sulfonate L, SCOP 3 mg/kg + Sodium Tanshinone IIA sulfonate 10 mg/kg, n=10), high dose Sodium Tanshinone IIA sulfonate group (Sodium Tanshinone IIA sulfonate H, SCOP 3 mg/kg + Sodium Tanshinone IIA sulfonate 20 mg/kg, n=10), and Donepezil group (DON, SCOP 3 mg/kg + ARI 3 mg/kg, n=10). Mice are treated with saline, Sodium Tanshinone IIA sulfonate, and Donepezil, respectively, by gavage, once per day for two weeks. SCOP is injected from the eighth day for one week (intraperitoneally, IP). The SCOP is injected 0.5 h before the Morris water maze test.
Rats[2]
Male Sprague-Dawley rats (200-250 g) are randomly divided into four groups by the random number table: 1) normoxia control group, 2) normoxia + Sodium Tanshinone IIA sulfonate group, 3) hypoxia control group, and 4) hypoxia + Sodium Tanshinone IIA sulfonate group. Groups 1 and 2 are placed in normoxic condition and groups 3 and 4 in a hypoxic cabin with normal pressure, as previously reported, where the oxygen concentration is maintained at 10±1%, in a sustained hypoxic condition for 21 days. Groups 2 and 4, starting from the first day of hypoxia, are, respectively, intraperitoneally injected with 30 mg/kg tanshinone IIA sulfonate; meanwhile, groups 1 and 3 receive the same dose of saline.

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
  • [1]. Xu QQ, et al. Sodium Tanshinone IIA Sulfonate Attenuates Scopolamine-Induced Cognitive Dysfunctions via Improving Cholinergic System. Biomed Res Int. 2016;2016:9852536

    [2]. Jiang Q, et al. Sodium tanshinone IIA sulfonate inhibits hypoxia-induced enhancement of SOCE in pulmonary arterial smooth muscle cells via the PKG-PPAR-γ signaling axis. Am J Physiol Cell Physiol. 2016 Jul 1;311(1):C136-49.

    [3]. Ouyang DS, et al. Kinetics of cytochrome P450 enzymes for metabolism of sodium tanshinone IIA sulfonate in vitro. Chin Med. 2016 Mar 22;11:11.

    [4]. Chen D, et al. Sodium tanshinone IIA sulfonate and its interactions with human CYP450s. Xenobiotica. 2016 Dec;46(12):1085-1092. Epub 2016 Mar 2.

    [5]. Lin S, et al. [Sodium tanshinone IIA sulfonate prevents postoperative peritoneal adhesions in rats by enhancing the activity of the peritoneal fibrinolytic system]. Nan Fang Yi Ke Da Xue Xue Bao. 2016 Feb;36(2):260-4.

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