规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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靶点 |
GSK-3β (IC50 = 5 nM); GSK-3β (IC50 = 60 nM)
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体外研究 (In Vitro) |
Tideglusib (NP031112) 治疗完全消除了星形胶质细胞和小胶质细胞培养物中谷氨酸处理后 TNF- 和 COX-2 表达的诱导。由于星形胶质细胞和小胶质细胞 24 小时暴露于该 TDZD 对细胞活力没有影响,因此 NP031112 的这些影响并不是由细胞活力降低引起的[2]。
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体内研究 (In Vivo) |
Tideglusib (NP031112) (50 mg/kg) 注射到大鼠海马中可显着减少红藻氨酸诱导的炎症(通过使用 T2 加权磁共振成像和神经胶质激活的水肿形成来测量),并且对海马受损区域具有神经保护作用。 2]。
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酶活实验 |
将 55 μM 的 [35S]Tideglusib (207 Bq/nmol) 与 5 μM GSK-3β 在 315 μL 50 mM Tris-HCl(pH 7.5,含有 150 mM NaCl 和 0.1 mM EGTA)中于 25 °C 孵育 1 小时。添加 35 μL 相同缓冲液(含或不含 100 mM DTE)后,孵育再延长 30 分钟。最后,将每个原始样品的第三份 40 μL 等分试样与 10 μL 不含还原剂的变性电泳样品缓冲液混合,并将 35 μL 该混合物上样到 10% 聚丙烯酰胺凝胶上,进行 SDS-PAGE,然后进行荧光照相干燥的凝胶。最后,将每个原始样品的第三个 40 L 等分试样与 10 L 不含还原剂的变性电泳样品缓冲液混合,并将 35 L 该混合物上样到 10% 聚丙烯酰胺凝胶上,进行 SDS-PAGE,然后进行荧光成像干燥的凝胶。
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细胞实验 |
用指定浓度的药物处理细胞24小时。
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动物实验 |
Rats; In this study, adult male Wistar rats (8–12 weeks old) are used. Rats (n≥5) are put into a stereotaxic machine. The hippocampus is given an injection of KA (1 μg in 2.5 μL l PBS) alone or in conjunction with Tideglusib (2 ng in 2.5 μL PBS). Animals in the control group are given vehicle injections and are the same age.
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参考文献 |
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分子式 |
C19H14N2O2S
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分子量 |
334.3917
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精确质量 |
334.0776
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元素分析 |
C, 68.25; H, 4.22; N, 8.38; O, 9.57; S, 9.59
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CAS号 |
865854-05-3
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相关CAS号 |
865854-05-3
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外观&性状 |
Solid powder
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SMILES |
C1=CC=C(C=C1)CN2C(=O)N(SC2=O)C3=CC=CC4=CC=CC=C43
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InChi Key |
PMJIHLSCWIDGMD-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C19H14N2O2S/c22-18-20(13-14-7-2-1-3-8-14)19(23)24-21(18)17-12-6-10-15-9-4-5-11-16(15)17/h1-12H,13H2
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化学名 |
4-benzyl-2-naphthalen-1-yl-1,2,4-thiadiazolidine-3,5-dione
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别名 |
Tideglusib; NP031112, NP-12; NP031112; NP 031112; NP-031112
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
DMSO: ~66 mg/mL (~197.4 mM)
Water: <1 mg/mL Ethanol: <1 mg/mL |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.48 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 4% DMSO+corn oil: 2.5mg/mL 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.9905 mL | 14.9526 mL | 29.9052 mL | |
5 mM | 0.5981 mL | 2.9905 mL | 5.9810 mL | |
10 mM | 0.2991 mL | 1.4953 mL | 2.9905 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Status | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05004129 | Recruiting | Drug: Tideglusib | Congenital Myotonic Dystrophy | AMO Pharma Limited | August 23, 2021 | Phase 2 Phase 3 |
NCT05105958 | Not yet recruiting | Drug: Tideglusib | Amyotrophic Lateral Sclerosis | University Hospital, Geneva | December 1, 2025 | Phase 2 |
NCT02858908 | Completed | Drug: Tideglusib | Myotonic Dystrophy 1 | AMO Pharma Limited | July 20, 2016 | Phase 2 |
NCT01350362 | Completed | Drug: tideglusib Drug: Placebo |
Alzheimer's Disease | Noscira SA | April 2011 | Phase 2 |
NCT00948259 | Completed | Drug: NP031112 Drug: Placebo |
Alzheimer´s Disease | Noscira SA | December 2008 | Phase 1 Phase 2 |
Inhibition of PI3K pathway signaling in cells. KPL-4 cells were treated with the indicated concentrations of CH5132799 for 2 hours. Clin Cancer Res, 2011, 17(10), 3272-3281. td> |
Antitumor activity in mouse xenograft models of cell lines harboring genetic alterations, including PIK3CA mutations |
Antitumor activity in combination with trastuzumab in the trastuzumab-insensitive model. |