|2,2'-二硫代二基二乙胺二盐酸盐|CsnPharm

CAS No.: 56-17-7

胱胺二盐酸盐 Catalog No. CSN22548

Synonyms: Decarboxycystine dihydrochloride;2-Aminoethyl disulfide dihydrochloride;2

Cystamine 2HCl can inhibit transglutaminase and interrupt with sulfhydryl enzymes. It is used as a radiation-protective agent, eparin antagonist and thiol modification reagent.

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实验方案

技术信息

生物活性

描述TG2 (transglutaminase 2) mediates covalent cross‐links of structural proteins, acts as a G-protein (G_h) in transmembrane signalling and is involved in cell proliferation, cell adhesion, apoptosis, cell–matrix interactions and reorganization of extracellular matrix. Cystamine have been shown to be neuroprotective, to increase survival, to improve motor performance in Huntington's disease and to reduce neuronal loss in animal models of Parkinson's disease. The therapeutic benefits mediated by cystamine have, in part, been attributed to inhibition of TG2^[1]. Cystamine concentration-dependently inhibited responses to phenylephrine, 5-HT and U46619 and for extracellular potassium. Cystamine relaxed and reduced [Ca²⁺]_i in phenylephrine-contracted arteries. In potassium-contracted arteries, cystamine induced less relaxation without changing [Ca²⁺]_i, and these relaxations were blocked by mitochondrial complex inhibitors. Cystamine induced vasodilatation by inhibition of receptor-coupled TG2, leading to opening of K_v channels and reduction of intracellular calcium, and by activation of a pathway sensitive to inhibitors of the mitochondrial complexes I and III. Both pathways may contribute to the antihypertensive and neuroprotective effect of cystamine^[1]. Cystamine has been shown to cause marked suppression of HIV replication in cultured lymphocytes and macrophages^[2]. CD studies showed the interesting ability of cystamine to shift the equilibrium B/A-DNA towards the B-form^[3]. In vivo, treatment of chronically infected macrophages with cystamine, at a concentration (500 µM) that did not show any cytotoxic or cytostatic effects, strongly decreased (> 80%) HIV-p24 antigen production and completely abolished the production of infectious viral particles^[4].
动物研究
剂量
Mice: 10 mg/kg - 200 mg/kg^[1] (i.p.) Rat: 30 mg/kg, 60 mg/kg^[2] (p.o.)

给药途径
i.p., p.o.
参考文献

动物研究
剂量	Mice: 10 mg/kg - 200 mg/kg^[1] (i.p.) Rat: 30 mg/kg, 60 mg/kg^[2] (p.o.)
给药途径	i.p., p.o.

[1] Engholm M, Pinilla E, Mogensen S, Matchkov V, Hedegaard ER, Chen H, Mulvany MJ, Simonsen U. Involvement of transglutaminase 2 and voltage-gated potassium channels in cystamine vasodilatation in rat mesenteric small arteries. Br J Pharmacol. 2016 Mar;173(5):839-55. doi: 10.1111/bph.13393. Epub 2016 Jan 27. PMID: 26603619; PMCID: PMC4761098.
[2] Toohey JI. Sulfur metabolism in AIDS: cystamine as an anti-HIV agent. AIDS Res Hum Retroviruses. 2009 Nov;25(11):1057-60. doi: 10.1089/aid.2009.0091. PMID: 19886835.
[3] Allegra P, Amodeo E, Colombatto S, Solinas SP. The ability of cystamine to bind DNA. Amino Acids. 2002;22(2):155-66. doi: 10.1007/s007260200004. PMID: 12395183.
[4] Bergamini A, Capozzi M, Ghibelli L, Dini L, Salanitro A, Milanese G, Wagner T, Beninati S, Pesce CD, Amici C, et al. Cystamine potently suppresses in vitro HIV replication in acutely and chronically infected human cells. J Clin Invest. 1994 May;93(5):2251-7. doi: 10.1172/JCI117223. PMID: 8182157; PMCID: PMC294379.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.4404 mL
- 22.2022 mL
- 44.4043 mL
- 5 mM
- 0.8881 mL
- 4.4404 mL
- 8.8809 mL
- 10 mM
- 0.4440 mL
- 2.2202 mL
- 4.4404 mL

技术信息

CAS号

56-17-7

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C4H14Cl2N2S2

运输

蓝冰

分子量

225.20

别名

Decarboxycystine dihydrochloride;2-Aminoethyl disulfide dihydrochloride;2;2'-Dithiobisethanamine dihydrochloride;Decarboxycystine 2HCl;2-Aminoethyl disulfide 2HCl;2,2\'-Dithiobisethanamine 2HCl

溶解度

DMSO	14.0 mg/mL (62.2 mM)
Ethanol	2.0 mg/mL (8.9 mM)

动物实验配方

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胱胺二盐酸盐 Catalog No. CSN22548

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