(S)-(+)-Dimethindene maleate
目录号 : GC14479
(S)-(+)-Dimethindene maleate是一种具有高效选择性的毒蕈碱M2受体拮抗剂（pA2 = 7.86/7.74; pKi = 7.78）。
Cas No.:136152-65-3
Sample solution is provided at 25 µL, 10mM.
(S)-(+)-Dimethindene maleate is a highly selective muscarinic M2 receptor antagonist (pA2 = 7.86/7.74; pKi= 7.78)[1]. The muscarinic M2 receptor is a G protein-coupled receptor primarily distributed in the heart, and its activation can inhibit heart rate and myocardial contractility[2]. (S)-(+)-Dimethindene maleate is commonly used in research areas such as autonomic nervous regulation, cardiovascular and respiratory systems, and can assist other chemicals in creating extended pluripotent stem cells (EPSCs)[3,4].
In vitro, reprogramming goat fetal fibroblasts (GFFs) using LCDM medium containing (S)-(+)-Dimethindene maleate (2µM) successfully induced the generation of pluripotent goat induced pluripotent stem cells (giPSCs), which were capable of differentiating into the three germ layers in vitro[5]. Pretreatment of rabbit vas deferens with (S)-(+)-Dimethindene maleate (10µM) for 30-60min competitively antagonized the 4-Cl-McN-A-343-induced inhibition of neurogenic twitch contractions[1]. Culture of mouse embryonic stem cells (mESCs) for 3 days in LCDM medium containing (S)-(+)-Dimethindene maleate (2µM) converted them into mouse extended pluripotent stem cells (mEPSCs), and this medium could be used for subsequent routine passaging and culture[6].
References:
[1] Pfaff O, Hildebrandt C, Waelbroeck M, et al. The (S)-(+)-enantiomer of dimethindene: a novel M2-selective muscarinic receptor antagonist[J]. European Journal of Pharmacology, 1995, 286(3): 229-240.
[2] Saternos H C, Almarghalani D A, Gibson H M, et al. Distribution and function of the muscarinic receptor subtypes in the cardiovascular system[J]. Physiological Genomics, 2018, 50(1): 1-9.
[3] Xu J, Yu L, Guo J, et al. Generation of pig induced pluripotent stem cells using an extended pluripotent stem cell culture system[J]. Stem Cell Research & Therapy, 2019, 10(1): 193.
[4] Lanzafame A A, Christopoulos A, Mitchelson F. Cellular signaling mechanisms for muscarinic acetylcholine receptors[J]. Receptors and Channels, 2003, 9(4): 241-260.
[5] Liu F, Wang J, Yue Y, et al. Derivation of arbas cashmere goat induced pluripotent stem cells in LCDM with trophectoderm lineage differentiation and interspecies chimeric abilities[J]. International Journal of Molecular Sciences, 2023, 24(19): 14728.
[6] Zhu K, Liu Y, Fan C, et al. Etv5 safeguards trophoblast stem cells differentiation from mouse EPSCs by regulating fibroblast growth factor receptor 2[J]. Molecular Biology Reports, 2020, 47(12): 9259-9269.
(S)-(+)-Dimethindene maleate是一种具有高效选择性的毒蕈碱M2受体拮抗剂（pA2 = 7.86/7.74; pKi = 7.78）[1]。毒蕈碱M2受体是一种G蛋白偶联受体，主要分布于心脏，激活后能抑制心率和心肌收缩力[2]。(S)-(+)-Dimethindene maleate通常用于自主神经调节、心血管与呼吸系统等领域的研究，并可辅助其他化学物质以创建扩展多能干细胞（EPS）[3,4]。
在体外，用含有(S)-(+)-Dimethindene maleate（2μM）的LCDM培养基对山羊胎儿成纤维细胞（GFFs）进行重编程，成功诱导出具有多能性的山羊诱导多能干细胞（giPSCs），并能在体外分化为三个胚层[5]。(S)-(+)-Dimethindene maleate（10μM）预处理兔输精管30-60min，竞争性地拮抗了由4-Cl-McN-A-343诱导的神经源性抽搐抑制[1]。用含有(S)-(+)-Dimethindene maleate（2μM）的LCDM培养基培养小鼠胚胎干细胞（mESCs）3天，可将其转化为小鼠扩展多能干细胞（mEPSCs），并可使用该培养基进行后续的常规传代培养[6]。
| Cell experiment [1]: | |
Cell lines | Goat fetal fibroblasts (GFFs) |
Preparation Method | The GFFs were cultured in the 6cm dishes under 5% CO2 at 38.5℃, and the medium was changed every day. When the cell densities reached approximately 90%, the GFFs were passaged. The PiggyBac plasmid and PiggyBac transposase vector were co-transfected into the GFFs by electroporation (approximately 106 cells per electro-transfection). The GFFs were then plated at a density of 5000 cells per well in 12-well plates seeded with mitomycin C-treated mouse embryonic fibroblast cells and cultured in DMEM medium supplemented with 20% FBS under 5% CO2 at 38.5℃. The medium was switched to the LCDM medium (with 2μM (S)-(+)-Dimethindene maleate) a day later. giPSCs were passaged every 3-4 days, and the medium was changed every day. |
Reaction Conditions | 2μM |
Applications | LCDM medium (with 2μM (S)-(+)-Dimethindene maleate) can be used to derive giPSCs and maintain their pluripotency. |
References: | |
| Cas No. | 136152-65-3 | SDF | |
| 化学名 | (S)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)-1H-inden-2-yl)ethanamine maleate | ||
| Canonical SMILES | OC(/C=C\C(O)=O)=O.C[C@H](C1=NC=CC=C1)C2=C(CCN(C)C)CC3=CC=CC=C23 | ||
| 分子式 | C20H24N2.C4H4O4 | 分子量 | 408.5 |
| 溶解度 | ≥ 20.45mg/mL in Water | 储存条件 | Store at -20°C |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.448 mL | 12.2399 mL | 24.4798 mL |
| 5 mM | 489.6 μL | 2.448 mL | 4.896 mL |
| 10 mM | 244.8 μL | 1.224 mL | 2.448 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
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