| 规格 | 价格 | 库存 | 数量 |
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| 10 mM * 1 mL in DMSO |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| Other Sizes |
| 靶点 |
Acetylcholinesterase/AChE
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|---|---|
| 体外研究 (In Vitro) |
乙酰胆碱酯酶抑制剂，包括新斯的明，已被用于拮抗神经肌肉阻滞多年。Sugammadex使用其γ-环糊精环逆转这种阻断，这种机制不同于胆碱酯酶，因此可以避免新斯的明的副作用。尽管在几项临床研究中已经概述了Sugammadex相对于新斯的明的优越性，但据我们所知，还没有任何关于细胞培养的研究来比较这两种药物的细胞毒性、遗传毒性和凋亡作用。因此，这是第一项比较不同剂量两种药物对人胚胎肾（HEK-293）细胞的细胞毒性、遗传毒性和凋亡作用的研究。在这项研究中，分别使用MTT、彗星试验和流式细胞术膜联蛋白-V方法分析了Sugammadex和新斯的明对HEK-293细胞的细胞毒性、遗传毒性和凋亡作用。结果表明，50、100、250和500µg/mL的新斯的明比同等剂量的Sugammadex具有更强的细胞毒性。发现500和1000µg/mL的新斯的明具有更高的遗传毒性，500µg/mL的新斯的明引起细胞凋亡和坏死的风险在统计学上高于Sugammadex（p＜0.05）。与Sugammadex相同剂量的新斯的明体外给药对HEK-293细胞具有更大的细胞毒性、遗传毒性和凋亡作用[1]。
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| 体内研究 (In Vivo) |
在慢性炎症性疾病（如哮喘）期间，白细胞可以侵入中枢神经系统（CNS），并与CNS驻留细胞一起产生过量的活性氧（ROS）产生以及抗氧化系统失衡，导致氧化应激，这在很大程度上导致了神经炎症。从这个意义上讲，本研究的目的是研究以控制肺部炎症能力而闻名的新斯的明治疗对哮喘小鼠大脑皮层氧化应激的影响。将雌性BALB/cJ小鼠置于卵清蛋白（OVA）诱导的哮喘模型中。对照组仅接受杜尔贝科磷酸缓冲盐水（DPBS）。为了评估新斯的明的效果，小鼠在每次OVA攻击后30分钟腹腔注射80μg/kg的新斯的明。我们的研究结果首次表明，新斯的明（一种不穿过血脑屏障的乙酰胆碱酯酶抑制剂）治疗能够恢复哮喘小鼠大脑皮层中ROS的产生并改变抗氧化酶过氧化氢酶。这些结果支持外周免疫系统和中枢神经系统之间的沟通，并表明乙酰胆碱酯酶抑制剂，如新斯的明，应作为哮喘神经保护的可能治疗策略进行进一步研究[2]。
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| 动物实验 |
Sensitization, airway challenge and neostigmine treatment[2]
The animals were sensitized by subcutaneous injections of 20 μg ovalbumin (OVA), diluted (200 μL) in Dulbecco’s phosphate-buffered saline (DPBS), on days 0 and 7, followed by three intranasal challenges with 100 μg of OVA, diluted in DPBS (50 μL), on days 14, 15, and 16 of the protocol. The control group received only DPBS in the sensitization and intranasal challenges. To evaluate neostigmine effects on the oxidative stress in the cerebral cortex, the mice received 80 μg/kg of neostigmine treatment intraperitoneally (Hofer et al. 2008) once a day during three consecutive days (14, 15, and 16) 30 min after of OVA challenge. On day 17 of the protocol, animals were anesthetized by intraperitoneal injection solution of ketamine (0.4 mg/g) and xylazine (0.2 mg/g) followed euthanasia by heart puncture exsanguination. Bronchoalveolar lavage (BAL), lung tissue and cerebral cortex for analyzes were collected. The study protocol is illustrated in Fig. 1. |
| 毒性/毒理 (Toxicokinetics/TK) |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Limited data indicate that use of neostigmine to treat myasthenia gravis may be acceptable during breastfeeding, although pyridostigmine may be preferred. Monitor newborns because abdominal cramps after each breastfeeding has been reported. Because of its short half-life, single doses of neostigmine to reverse neuromuscular blockade following surgery are unlikely to adversely affect the breastfed infant more than transiently. ◉ Effects in Breastfed Infants Six infants of mothers treated with neostigmine for myasthenia gravis were reportedly breastfed successfully. One newborn infant appeared to have abdominal cramps after each breastfeeding, probably caused by neostigmine, although it could not be detected in the breastmilk of the infant's mother. ◉ Effects on Lactation and Breastmilk Relevant published information in nursing mothers was not found as of the revision date. In animals, cholinergic drugs increase oxytocin release, and have variable effects on serum prolactin. The prolactin level in a mother with established lactation may not affect her ability to breastfeed. |
| 参考文献 |
[1].Comparison of the cytotoxic, genotoxic and apoptotic effects of Sugammadex and Neostigmine on human embryonic renal cell (HEK-293). Cell Mol Biol (Noisy-le-grand). 2018 Oct 30;64(13):74-78.
[2].Neostigmine treatment induces neuroprotection against oxidative stress in cerebral cortex of asthmatic mice. Metab Brain Dis. 2020 Jun;35(5):765-774. [3]. Clin Colon Rectal Surg.2005 May;18(2):96-101. |
| 其他信息 |
Neostigmine methyl sulfate is an arylammonium sulfate salt. It has a role as an EC 3.1.1.8 (cholinesterase) inhibitor.
A cholinesterase inhibitor used in the treatment of myasthenia gravis and to reverse the effects of muscle relaxants such as gallamine and tubocurarine. Neostigmine, unlike PHYSOSTIGMINE, does not cross the blood-brain barrier. See also: Neostigmine (has active moiety); Glycopyrrolate; neostigmine methylsulfate (component of). |
| 分子式 |
C13H22N2O6S
|
|---|---|
| 分子量 |
334.387
|
| 精确质量 |
334.119
|
| 元素分析 |
C, 46.70; H, 6.63; N, 8.38; O, 28.71; S, 9.59
|
| CAS号 |
51-60-5
|
| 相关CAS号 |
Neostigmine Bromide;114-80-7; 114-80-7 (bromide); 1212-37-9 (iodide); 59-99-4 (cation); 51-60-5 (methylsulfate); 588-17-0 (hydroxide)
|
| PubChem CID |
5824
|
| 外观&性状 |
White to off-white solid powder
|
| 沸点 |
457ºC
|
| 熔点 |
175-177 °C(lit.)
|
| LogP |
2.117
|
| tPSA |
104.35
|
| 氢键供体(HBD)数目 |
0
|
| 氢键受体(HBA)数目 |
6
|
| 可旋转键数目(RBC) |
3
|
| 重原子数目 |
22
|
| 分子复杂度/Complexity |
337
|
| 定义原子立体中心数目 |
0
|
| SMILES |
S(=O)(=O)([O-])OC([H])([H])[H].O(C(N(C([H])([H])[H])C([H])([H])[H])=O)C1=C([H])C([H])=C([H])C(=C1[H])[N+](C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H]
|
| InChi Key |
3-((dimethylcarbamoyl)oxy)-N,N,N-trimethylbenzenaminium methyl sulfate
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| InChi Code |
OSZNNLWOYWAHSS-UHFFFAOYSA-M SMILES
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| 化学名 |
Neostigmine, Prostigmin, Vagostigmin, Polstigmine Neostigmine methylsulfate
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| 别名 |
Prostigmin; Neostigmine; Neostigmine methyl sulfate; 51-60-5; NEOSTIGMINE METHYLSULFATE; Syntostigmin; Hodostin; Neostigmine methylsulphate; Neostigmeth; Synstigmine; Polstigmine; Neostigmine methylsulfate; Vagostigmin
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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 注意： 请将本产品存放在密封且受保护的环境中（例如氮气保护），避免吸湿/受潮和光照。 |
| 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)
|
| 溶解度 (体外实验) |
DMSO : ≥ 100 mg/mL (~299.05 mM)
H2O : ~100 mg/mL (~299.05 mM) |
|---|---|
| 溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 2.5 mg/mL (7.48 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。 *生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。 配方 2 中的溶解度: ≥ 2.5 mg/mL (7.48 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。 例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中，混匀。 *20% SBE-β-CD 生理盐水溶液的制备（4°C，1 周）：将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中，得到澄清溶液。 View More
配方 3 中的溶解度: ≥ 2.5 mg/mL (7.48 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。 配方 4 中的溶解度: 100 mg/mL (299.05 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶. 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 | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03316963 | TERMINATED | Drug: Neostigmine Methylsulfate | Snoring | Emory University | 2017-11-14 | Early Phase 1 |
| NCT05724550 | RECRUITING | Drug: Sugammadex Drug: Neostigmine |
Neuromuscular Block, Residual | Seoul National University Hospital | 2023-02-22 | Not Applicable |
| NCT03587441 | COMPLETED | Drug: Neostigmine Methylsulfate Drug: Dextrose 5% in water |
Post-Dural Puncture Headache | Fayoum University Hospital | 2018-08-04 | Phase 4 |
| NCT01050543 | COMPLETEDWITH RESULTS | Drug: sugammadex Drug: neostigmine |
Neuromuscular Blockade | Merck Sharp & Dohme LLC | 2010-02-01 | Phase 3 |
| NCT02279147 | UNKNOWN STATUS | Drug: neostigmine methylsulfate， raceanisodamine hydrochloride |
Jaundice, Obstructive Systemic Inflammatory Response Syndrome |
Wanqing Gu | 2014-08 | Phase 1 Phase 2 |
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