Cysteamine (β-Mercaptoethylamine)
(Synonyms: 巯基乙胺) 目录号 : GC337792-Aminoethanethiol (cysteamine, β-Mercaptoethylamine, 2-Mercaptoethylamine, Thioethanolamine, Mercaptamine) is a radiation-protective agent that oxidizes in air to form cystamine.
Cas No.:60-23-1
Sample solution is provided at 25 µL, 10mM.
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2-Aminoethanethiol (cysteamine, β-Mercaptoethylamine, 2-Mercaptoethylamine, Thioethanolamine, Mercaptamine) is a radiation-protective agent that oxidizes in air to form cystamine.
Cas No. | 60-23-1 | SDF | |
别名 | 巯基乙胺 | ||
Canonical SMILES | NCCS | ||
分子式 | C2H7NS | 分子量 | 77.15 |
溶解度 | Water : 150 mg/mL (1944.26 mM) | 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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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 12.9618 mL | 64.8088 mL | 129.6176 mL |
5 mM | 2.5924 mL | 12.9618 mL | 25.9235 mL |
10 mM | 1.2962 mL | 6.4809 mL | 12.9618 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
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 | ||||||||||
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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,
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 saline,混匀澄清。
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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Topical Stabilized Cysteamine as a New Treatment for Hyperpigmentation Disorders: Melasma, Post-Inflammatory Hyperpigmentation, and Lentigines
J Drugs Dermatol 2021 Dec 1;20(12):1276-1279.PMID:34898155DOI:10.36849/jdd.6367.
Cysteamine is an aminothiol naturally present in cells of the human body as an antioxidant resulting from the degradation of Coenzyme A. Physiologically it is well distributed in mammalian tissues. Highly concentrated in human milk, Cysteamine acts as an intrinsic antioxidant and is known for its protective role. Multiple studies now document that Cysteamine is a potent skin depigmenting agent. Historically, its rapid oxidation and very offensive odor made it difficult for topical use until recently when stabilization of Cysteamine was achieved. This has led to an acceptable galenical form for topical application. Since 2015, the efficacy, safety, and tolerability of stabilized Cysteamine (st.Cys) has been demonstrated in multiple clinical studies, as well a case reports. Stabilized Cysteamine has demonstrated significant effectiveness for the treatment of melasma by two double-blind randomized and vehicle control trials. Stabilized Cysteamine (st.Cys) has shown to be as effective as well-known depigmenting therapies, including triple combination cream or tranexamic acid mesotherapy, with higher tolerability. A recent clinical trial has shown considerable efficacy of topical Cysteamine for the treatment of senile lentigines, which are usually considered to be resistant to topical depigmenting agents. Topical stabilized Cysteamine can be regarded to as one of the most potent treatments available for hyperpigmentation disorders in humans. J Drugs Dermatol. 2021;20(12): 1276-1279. doi:10.36849/JDD.6367.
Is Cysteamine use effective in the treatment of melasma? A systematic review and meta-analysis
Dermatol Ther 2022 Dec;35(12):e15961.PMID:36285354DOI:10.1111/dth.15961.
Melasma is a recurrent hypermelanosis disorder characterized by the appearance of brownish and symmetrical spots on the skin. It affects the quality of life and is resistant to available treatment approaches. Cysteamine has been reported as a promising depigmenting agent for melasma treatment and following formulation enhancement, its use is being reported. This review aimed to evaluate the efficacy of the use of depigmenting formulations containing 5% Cysteamine in the treatment of patients with melasma. A systematic search was performed in PubMed, Science Direct, and Scielo databases until December 27, 2021, based on criteria selected by the Preferred Reporting Items for Systematic Reviews and Meta-Analyses guidelines. Statistical analysis was performed with Review Manager 5.4 software. The risk of bias was assessed using the Cochrane Risk of Bias Tool for Randomized Trials. A total of six studies containing 120 melasma patients treated with 5% Cysteamine were included in this meta-analysis. The meta-analysis demonstrated that 5% Cysteamine is effective for the treatment of patients with melasma (MD 6.26 [95% CI 3.68-8.83], p < 0.0001, I2 = 86%). In this review, through meta-analysis allows concluding that 5% Cysteamine is effective in the treatment of melasma and presents a low probability of side or adverse effects.
Cysteamine: an old drug with new potential
Drug Discov Today 2013 Aug;18(15-16):785-92.PMID:23416144DOI:10.1016/j.drudis.2013.02.003.
Cysteamine is an amino thiol with the chemical formula HSCH2CH2NH2. Endogenously, Cysteamine is derived from coenzyme A degradation, although its plasma concentrations are low. Most experience with Cysteamine as a drug originates from the field of the orphan disease cystinosis, in which Cysteamine is prescribed to decrease intralysosomal cystine accumulation. However, over the years, the drug has been used for several other applications both in vitro and in vivo. In this article, we review the different applications of Cysteamine, ending with an overview of ongoing clinical trials for new indications, such as neurodegenerative disorders and nonalcoholic fatty liver disease (NAFLD). The recent development of an enteric-coated Cysteamine formulation makes Cysteamine more patient friendly and will extend its applicability for both old and new indications.
Cystamine and Cysteamine as inhibitors of transglutaminase activity in vivo
Biosci Rep 2018 Sep 5;38(5):BSR20180691.PMID:30054429DOI:10.1042/BSR20180691.
Cystamine is commonly used as a transglutaminase inhibitor. This disulphide undergoes reduction in vivo to the aminothiol compound, Cysteamine. Thus, the mechanism by which cystamine inhibits transglutaminase activity in vivo could be due to either cystamine or Cysteamine, which depends on the local redox environment. Cystamine inactivates transglutaminases by promoting the oxidation of two vicinal cysteine residues on the enzyme to an allosteric disulphide, whereas Cysteamine acts as a competitive inhibitor for transamidation reactions catalyzed by this enzyme. The latter mechanism is likely to result in the formation of a unique biomarker, N-(γ-glutamyl)Cysteamine that could serve to indicate how cyst(e)amine acts to inhibit transglutaminases inside cells and the body.
Cysteamine as a novel disease-modifying compound for Parkinson's disease: Over a decade of research supporting a clinical trial
Neurobiol Dis 2019 Oct;130:104530.PMID:31301344DOI:10.1016/j.nbd.2019.104530.
To date, medical and surgical interventions offered to patients with Parkinson's disease (PD) serve only to manage clinical symptoms; they have not shown the capacity to halt nor reverse degenerative processes. There is therefore an urgent need to identify and/or develop therapeutic strategies that will demonstrate 'disease modifying' capacities. The molecule cystamine, and its reduced form Cysteamine, act via a number of pathways determined to be critical to the pathogenesis of PD. In particular, cystamine is capable of crossing the blood-brain barrier, and both agents (cystamine and Cysteamine) can promote the secretion of neurotrophic factors, inhibit oxidative stress, reduce inflammatory responses and importantly, have already been trialed in humans for a number of other clinical indications. In the last decade, our laboratory has accumulated compelling evidence that both cystamine and Cysteamine can halt, and even reverse, ongoing neurodegenerative processes in a number of different models of PD, and as such, should now be taken forward to clinical trials in PD.