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CPI-1189
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
CPI-1189图片
CAS NO:183619-38-7
包装与价格：
包装价格(元)
5mg电议
25mg电议

产品介绍
CPI-1189 是一种 TNF-α 释放抑制剂，具有抗氧化和神经保护特性。
Cas No.183619-38-7
别名N-叔丁基-4-乙酰氨基苯甲酰胺
化学名(Z)-N-(4-(tert-butylcarbamoyl)phenyl)acetimidic acid
Canonical SMILESC/C(O)=N/C1=CC=C(C=C1)C(NC(C)(C)C)=O
分子式C13H18N2O2
分子量234.29
溶解度≥ 23.4mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

CPI-1189 is a proapoptotic cytokine tumor necrosis factor (TNF) alpha inhibitor.

AIDS dementia complex is characterized by increased gliosis, apoptosis, and oxidative stress in the CNS, as well as a compromised blood-brain barrier. TNF-alpha has been reported to be elevated in AIDS dementia complex brains and may contribute to AIDS dementia complex.

In vitro: CPI-1189 could potently inhibit p38-MAPK phosphorylation displaying protective action against tumor necrosis factor-alpha (TNFalpha)-induced neurodegeneration. Moreover, in primary astrocytes treated with interleukin 1beta, CPI-1189 inhibited p38-MAPK phosphorylation at low concentrations [1].

In vivo: To model elevated TNF-alpha in AIDS dementia complex, TNF-alpha was infused into rats. Results showed that the co-administration of CPI-1189 prevented TNF-alpha induced apoptosis. Both TNF-alpha and CPI-1189 treatment could suppress glial fibrillary acidic protein staining. TNF-alpha alone did not affect the integrity of the blood-brain barrier significantly, but CPI-1189 treatment increased blood-brain barrier integrity [2].

Clinical trial: Previous clinical study showed that CPI-1189 was well tolerated, with 91% of CPI-1189-treated subjects and 76% of placebo-treated subjects completing the trial. Skin rash was equally found in placebo and drug-treated arms. One subject developed a cataract on CPI-1189. CD4 lymphocyte counts and plasma HIV viral load remained stable in all groups throughout the trial [3].

References:
[1] Hensley K,Robinson KA,Pye QN,Floyd RA,Cheng I,Garland WA,Irwin I.  CPI-1189 inhibits interleukin 1beta-induced p38-mitogen-activated protein kinase phosphorylation: an explanation for its neuroprotective properties Neurosci Lett.2000 Mar 10;281(2-3):179-82.
[2] Bjugstad KB,Flitter WD,Garland WA,Philpot RM,Kirstein CL,Arendash GW.  CPI-1189 prevents apoptosis and reduces glial fibrillary acidic protein immunostaining in a TNF-alpha infusion model for AIDS dementia complex. J Neurovirol.2000 Dec;6(6):478-91.
[3] Clifford DB,McArthur JC,Schifitto G,Kieburtz K,McDermott MP,Letendre S,Cohen BA,Marder K,Ellis RJ,Marra CM;Neurologic AIDS Research Consortium.  A randomized clinical trial of CPI-1189 for HIV-associated cognitive-motor impairment. Neurology.2002 Nov 26;59(10):1568-73.