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Cystamine (dihydrochloride)

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Chemical Structure| 56-17-7 同义名 : Cystamine dihydrochloride;Cystamine (hydrochloride)
CAS号 : 56-17-7
货号 : A210400
分子式 : C4H14Cl2N2S2
纯度 : 98%
分子量 : 225.203
MDL号 : MFCD00012905
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(466.25 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 100 mg/mL(444.04 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 TG2 (transglutaminase 2) mediates covalent cross‐links of structural proteins, acts as a G-protein (Gh) 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 Kv 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.44mL

0.89mL

0.44mL

22.20mL

4.44mL

2.22mL

44.40mL

8.88mL

4.44mL

参考文献

[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.