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MJ33

MJ33用途

MJ33 是一种活性位点定向的、特异的、竞争性的和可逆性的磷脂酶 A2 (PLA2) 抑制剂。MJ33 阻断 Prdx6 的非钙依赖性磷脂酶A2 (iPLA2) 活性。MJ33 对炎症性脑损伤有重要作用。

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MJ33名称

[ CAS 号 ]:
199106-13-3

[ 中文名 ]:
MJ33 锂盐

[ 英文名 ]:
MJ33

[英文别名 ]:

IN1224
MJ33 lithium salt
MJ33
mj33 lithium salt

MJ33生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 磷脂

研究领域 >> 炎症/免疫

[体外研究]

MJ33是PLA2的过渡态类似竞争性抑制剂,在全肺和分离的肺泡2型细胞中抑制了50%的二棕榈酰磷脂酰胆碱(DPPC)的降解。MJ33在无钙培养基中pH值为4.0时,对肺匀浆或分离的2型细胞中PLA2活性的体外测定有明显的抑制作用,但对pH值为8.5时Ca2+依赖的PLA2活性没有影响[3]。

[体内研究]

MJ33(0.5μM/kg,经尾静脉,MCAO前24小时)显著阻断Prdx6-siRNA刺激大鼠IL-1β、IL-17和IL-23的升高[2]。与Prdx6-siRNA组相比,Prdx6-siRNA和MJ33联合暴露显著下调NF-κB、iNOS和COX-2的mRNA和蛋白表达[2]。动物模型：成年雄性Sprague-Dawley大鼠,体重270-310g(大脑中动脉闭塞(MCAO)组)[2]剂量：0.5μM/kg,尾静脉注射,MCAO前24小时。结果：明显阻断Prdx6-siRNA刺激大鼠IL-1β、IL-17和IL-23的升高。

[参考文献]

[1]. Shanshan Y, et al. Phospholipase A2 of Peroxiredoxin 6 Plays a Critical Role in Cerebral Ischemia/Reperfusion Inflammatory Injury. Front Cell Neurosci. 2017 Apr 5;11:99.

[2]. Moawad AR, et al. Deficiency of peroxiredoxin 6 or inhibition of its phospholipase A2 activity impair the in vitro sperm fertilizing competence in mice. Sci Rep. 2017 Oct 11;7(1):12994.

[3]. Fisher AB, et al. Altered lung phospholipid metabolism in mice with targeted deletion of lysosomal-type phospholipase A2. J Lipid Res. 2005 Jun;46(6):1248-56.

MJ33物理化学性质

[ 沸点 ]:
522.7ºC at 760 mmHg

[ 分子式 ]:
C₂₂H₄₄F₃O₇P

[ 分子量 ]:
498.48300

[ 闪点 ]:
269.9ºC

[ 精确质量 ]:
498.29100

[ PSA ]:
86.86000

[ LogP ]:
7.63340

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
2.5E-12mmHg at 25°C

[ 储存条件 ]:
2-8°C

MJ33MSDS

详细MSDS(安全技术说明书)

MJ33安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 安全声明 (欧洲) ]:
S22

[ 危险品运输编码 ]:
NONH for all modes of transport

MJ33文献

1-Cys peroxiredoxin, a bifunctional enzyme with glutathione peroxidase and phospholipase A2 activities.

J. Biol. Chem. 275 , 28421, (2000)

This report provides definitive evidence that the protein 1-Cys peroxiredoxin is a bifunctional ("moonlighting") enzyme with two distinct active sites. We have previously shown that human, rat, and bo...

Fisher, A.B., Dodia, C.

Am. J. Physiol. Cell Physiol. 280 , 748, (2001)

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