丹参酮IIA磺酸盐作用机制 - Medchemexpress - MCE中国

1、Product Data SheetTanshinone IIA sulfonate sodiumCat. No.: HY-N1370CAS No.: 69659-80-9分式: CHNaOS分量: 396.39作靶点: CRAC Channel作通路: Membrane Transporter/Ion Channel储存式: Powder -20C 3 years4C 2 years* 该产品在溶液状态不稳定，建议您现现配，即刻使。溶解性数据体外实验 DMSO : 100 mg/mL (252.28 mM; Need ultrasonic)H2O : 8.33 mg/mL (21.01 mM

2、; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 2.5228 mL 12.6138 mL 25.2277 mL5 mM 0.5046 mL 2.5228 mL 5.0455 mL10 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，建议您现现配，即刻使.体内实验 请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 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 的

3、储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.31 mM); Clear solution此案可获得 2.5 mg/mL (6.31 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，

4、混合均匀。BIOLOGICAL ACTIVITYPage 1 of 2 www.MedChemE物活性 Tanshinone IIA sulfonate sodiumtanshinone IIA 的衍物，为 SOCE 的抑制剂，于治疗管疾病。体外研究 Sodium Tanshinone IIA sulfonate (12.5 M) inhibits hypoxia-induced PKG and PPAR- downregulation in PASMCsand distal pulmonary arteries of rats. The suppressive effects of Sodi

5、um Tanshinone IIA sulfonate on TRPC1 andTRPC6 expression in hypoxic PASMCs can be prevented by specific knockdown PKG or PPAR-. The suppressiveeffects of Sodium Tanshinone IIA sulfonate on basal calcium concentration and SOCE in hypoxic PASMCs can bereversed by specific knockdown of PKG or PPAR-. PK

6、G-PPAR- signaling axis participates in the suppressive effectsof Sodium Tanshinone IIA sulfonate on proliferation in hypoxic PASMCs. PPAR- agonist promotes the protectiverole of Sodium Tanshinone IIA sulfonate on basal Ca2+i and SOCE in hypoxic PASMCs2. Sodium tanshinone IIAsulfonate inhibits the ac

7、tivity of CYP3A4 in a dose-dependent manner by the HLMs and CYP3A4 isoform. The KMand Vmax values of STS are 54.814.6 M and 0.90.1 nmol/mg protein/min, respectively, for the HLMs and 7.51.4M and 6.80.3 nmol/nmol P450/min, respectively, for CYP3A4. CYP1A2, CYP2A6, CYP2C9, CYP2D6, CYP2E1, andCYP2C19 s

8、how minimal or no effects on the metabolism of STS3. Sodium Tanshinone IIA sulfonate inhibits theactivity of CYP3A4 in a dose-dependent manner in the HLMs and CYP3A4 isoform. Sodium Tanshinone IIA sulfonateprimarily inhibits the activities of CYP3A4 in vitro, and Sodium Tanshinone IIA sulfonate has

9、the potential toperpetrate drug-drug interactions with other CYP3A4 substrates4.体内研究 Sodium Tanshinone IIA sulfonate (10 mg/kg, 20 mg/kg) and Donepezil shorten escape latency, increase crossingtimes of the original position of the platform, and increase the time spent in the target quadrant. Sodium

10、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 sulfonateincreases the activity of superoxide dismutase (SOD) and decreases the leve

11、ls of malondialdehyde (MDA) andreactive oxygen species (ROS) in hippocampus and cortex1. Sodium Tanshinone IIA sulfonate prevention (30mg/kg/day) alleviates hypoxia-induced characteristic changes in chronic hypoxia PH rat model2. SodiumTanshinone IIA sulfonate (20, 10, and 5 mg/kg, i.p.) effectively

12、 prevents peritoneal adhesion without affectinganastomotic 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 withloared TGF-1 and collagen I e

13、xpressions in the ischemic tissues5.PROTOCOLAnimal Mice1Administration 12 Male Kunming mice (KM, weighing 35-40 g) are maintained on standard laboratory conditions with free access towater and food. Mice are randomly divided into five groups: vehicle control group (CON, 0.9% saline, n=10),scopolamin

14、e group (SCOP, n=10), low dose Sodium Tanshinone IIA sulfonate group (Sodium Tanshinone IIAsulfonate L, SCOP 3 mg/kg + Sodium Tanshinone IIA sulfonate 10 mg/kg, n=10), high dose Sodium Tanshinone IIAsulfonate group (Sodium Tanshinone IIA sulfonate H, SCOP 3 mg/kg + Sodium Tanshinone IIA sulfonate 20

15、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 isinjected from the eighth day for one week (intraperitoneally, IP). The SCOP is injected

16、0.5 h before the Morris watermaze test.Rats2Male 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

17、group. Groups 1 and 2 are placed in normoxic condition and groups 3and 4 in a hypoxic cabin with normal pressure, as previously reported, where the oxygen concentration is maintainedat 101%, in a sustained hypoxic condition for 21 days. Groups 2 and 4, starting from the first day of hypoxia, are,res

18、pectively, intraperitoneally injected with 30 mg/kg tanshinone IIA sulfonate; meanwhile, groups 1 and 3 receivethe same dose of saline.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Page 2 of 3 www.MedChemE户使本产品发表的科研献 Oxid Med Cell Longev. 2020 Apr. J

19、Cell Mol Med. 2020 Jan 27.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Xu QQ, et al. Sodium Tanshinone IIA Sulfonate Attenuates Scopolamine-Induced Cognitive Dysfunctions via Improving Cholinergic System. Biomed ResInt. 2016;2016:98525362. Jiang Q, et al. Sodium tanshinone IIA sulfonate inhibits hypoxia-induced enhancement of SOCE in pulmonary arterial smooth muscle cells via the PKG-PPAR- 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 sod