Arimoclomol maleate (BRX-220)

A co-inducer of heat shock proteins

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1mg

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货号: ajce46448
CAS: 289893-26-1
别名: BRX-220
分子式: C18H24ClN3O7
分子量: 429.85
纯度: >98%
溶解度: DMSO: 250 mg/mL (581.60 mM); Water: 100 mg/mL (232.64 mM)
储存: Store at -20°C
库存: 现货

Background

Arimoclomol is a co-inducer of heat shock proteins (Hsps).^1,2 It increases pancreatic Hsp60 and Hsp70 levels, decreases malondialdehyde (MDA) and protein carbonyl levels, increases glutathione peroxidase (GPX) activity, and decreases Cu/Zn superoxide dismutase (SOD) activity in a rat model of cholecystokinin (CCK) octapeptide-induced acute pancreatitis when administered at a dose of 20 mg/kg.¹ Arimoclomol (10 mg/kg, i.p.) increases spinal cord levels of Hsp70 and Hsp90 and motoneuron survival, decreases disease severity, and increases lifespan in a Cu/Zn SOD mutant (SOD1^G93A) transgenic mouse model of amyotrophic lateral sclerosis (ALS).²

1.Rakonczay, Z., Jr., Iványi, B., Varga, I., et al.Nontoxic heat shock protein coinducer BRX-220 protects against acute pancreatitis in ratsFree Radic. Biol. Med.32(12)1283-1292(2002) 2.Kieran, D., Kalmer, B., Dick, J.R.T., et al.Treatment with arimoclomol, a coinducer of heat shock proteins, delays disease progression in ALS miceNat. Med.10(4)402-405(2004)

Protocol

Animal experiment:

Rats[1]Male Wistar rats weighing 240-270 g are used. The animals are kept at a constant room temperature of 25°C with a 12 h light-dark cycle, and are allowed free access to water and standard laboratory chow. The rats are fasted 18 h before the end of the experiment. In group B (n=6), 20 mg/kg Arimoclomol (BRX-220) is administered intragastrically, followed by 75 μg/kg CCK subcutaneously three times, after 1, 3, and 5 h. This whole procedure is repeated for 5 d. The animals in group AB (n=6) receive physiological saline intragastrically instead of Arimoclomol, but otherwise the protocol is the same as in group B. The animals are sacrificed by exsanguination through the abdominal aorta 12 h after the last CCK injection. Three untreated rats (A) are killed for HSP60 and 72 determinations. The pancreas is quickly removed, cleaned from fat and lymph nodes, weighed, and frozen at -70°C until use[1].

参考文献:

[1]. Rakonczay Z Jr, et al. Nontoxic heat shock protein coinducer BRX-220 protects against acute pancreatitis in rats. Free Radic Biol Med. 2002 Jun 15;32(12):1283-92.
[2]. Phukan J. Arimoclomol, a coinducer of heat shock proteins for the potential treatment of amyotrophic lateral sclerosis. IDrugs. 2010 Jul;13(7):482-96.