生物活性分子抑制剂Cysteamine hydrochloride(Synonyms: 半胱胺盐酸盐; 2-Aminoethanethiol hydrochloride; 2-Mercaptoethylamine hydrochloride)

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Cysteamine hydrochloride (Synonyms: 半胱胺盐酸盐; 2-Aminoethanethiol hydrochloride; 2-Mercaptoethylamine hydrochloride) 纯度: ≥98.0%

Cysteamine hydrochloride (2-Aminoethanethiol hydrochloride) 是一种可口服的,用于肾病型胱胺酸症得小分子药物,也可作为抗氧化剂。

Cysteamine hydrochloride(Synonyms: 半胱胺盐酸盐; 2-Aminoethanethiol hydrochloride; 2-Mercaptoethylamine hydrochloride)

Cysteamine hydrochloride Chemical Structure

CAS No. : 156-57-0

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生物活性

Cysteamine hydrochloride (2-Aminoethanethiol hydrochloride) is an orally active agent for the treatment of nephropathic cystinosis and an antioxidant.

IC50 & Target[1][2]

Human Endogenous Metabolite

 

体外研究
(In Vitro)

Cysteamine hydrochloride (2-Aminoethanethiol hydrochloride) has been shown to increase intracellular glutathione levels in cystinotic cells, thus restoring the altered redox state of the cells. Also increased rates of apoptosis in cystinotic cells, which are thought to be the result of increased caspase 3 and protein kinase Cε activity, is counteracted by Cysteamine hydrochloride administration. Cysteamine hydrochloride has antioxidant properties as a result of increasing glutathione production. Cysteamine hydrochloride is an excellent scavenger of OH and HOCl; it also reacts with H2O2. Cysteamine hydrochloride increases the production of several heat shock proteins (HSP), including the murine Hsp40. Cysteamine hydrochloride exerts a dose-dependent effect on the doxorubicin-induced death of cancer cells, measured in both HeLa cells and B16 cells, whereas Cysteamine hydrochloride treatment alone had no influence on cell survival. In addition, in a doxorubicin-resistant breast cancer cell line, the addition of Cysteamine hydrochloride to doxorubicin results in a dramatic increase in cell death[1].
Cysteamine hydrochloride (100 μM) significantly is able to increase the intracellular GSH levels and the percentage of embryos that developed to the blastocyst stage of culture matured oocytes[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

113.61

Formula

C2H8ClNS

CAS 号

156-57-0

中文名称

半胱胺盐酸盐;α-巯基乙胺盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
In Vitro: 

DMSO : 250 mg/mL (2200.51 mM; Need ultrasonic)

H2O : ≥ 50 mg/mL (440.10 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 8.8020 mL 44.0102 mL 88.0204 mL
5 mM 1.7604 mL 8.8020 mL 17.6041 mL
10 mM 0.8802 mL 4.4010 mL 8.8020 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;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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方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,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 100 mg/mL (880.20 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (18.31 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (18.31 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (18.31 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (18.31 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (18.31 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (18.31 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Besouw, M., et al., Cysteamine: an old drug with new potential. Drug Discov Today, 2013. 18(15-16): p. 785-92.

    [2]. de Matos, D.G., et al., Effect of cysteamine on glutathione level and developmental capacity of bovine oocyte matured in vitro. Mol Reprod Dev, 1995. 42(4): p. 432-6.

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