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产品名称 | Lipase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
XEN445 |
+++
endothelial lipase, IC50: 0.237 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
JZL184 |
++++
MAGL, IC50: 8 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Tanshinone IIA | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Orlistat | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Atglistatin |
++
ATGL, IC50: 0.7 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | The monoacylglycerol lipase (MAGL) is a serine hydrolase responsible for the degradation of 2-arachidonoyl glycerol (2-AG). MJN110 is a potent and selective MAGL inhibitor with an IC50 value of 9.1nM. In human prostate cancer PC3 cells, treatment with MJN110 for 4 hours inhibited MAGL with an IC50 value of ~1nM. MJN110 also potently inhibited the 2-AG hydrolysis of in mouse brain homogenates with an IC50 value of 2.1nM without affecting the hydrolysis of N-arachidonoyl ethanolamine up to 50μM. The oral treatment of MJN110 (0.5–5.0mg/kg) in mice dose-dependently inhibited MAGL expression in the brain and liver. It also inhibited MAGL in vivo when administered intraperitoneally with the maximal inhibition observed at 0.25mg/kg in the live and 1.0mg/kg in the brain. The oral administration of MJN110 led to a 2-fold increase in 2-AG at the dose of 0.5mg/kg and a 10-fold increase at 5.0mg/kg. MJN110-treated mice also showed dose-dependent reduction of arachidonic acid in the brain[1]. |
作用机制 | MJN110 inhibits MAGL via the carbamylation of MAGL’s active-site serine nucleophile[1]. |
Dose | Rat: 5 mg/kg - 20 mg/kg[1] (i.p.) Mice: 0.0818 mg/kg - 0.143 mg/kg[2] (i.p.), 5 mg/kg[3] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.16mL 0.43mL 0.22mL |
10.81mL 2.16mL 1.08mL |
21.63mL 4.33mL 2.16mL |
CAS号 | 1438416-21-7 |
分子式 | C22H21Cl2N3O4 |
分子量 | 462.326 |
别名 | 2,5-Dioxopyrrolidin-1-yl 4-[bis(4-chlorophenyl)methyl]piperazine-1-carboxylate |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 250 mg/mL(540.74 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 |
动物实验配方 |