1210004-12-8
中文名稱
4-硝基苯基4-(3-苯氧基芐基)哌嗪-1-甲酸叔丁酯
英文名稱
JZL 195
CAS
1210004-12-8
分子式
C24H23N3O5
分子量
433.46
MOL 文件
1210004-12-8.mol
更新日期
2024/10/28 15:28:30
1210004-12-8 結(jié)構(gòu)式
基本信息
中文別名
4-硝基苯基4-(3-苯氧基芐基)哌嗪-1-甲酸叔丁酯 英文別名
CS-1586JZL 195
JZL-195
JZL 195
JZL195
4-nitrophenyl 4-(3-phenoxybenzyl)piperazine-1-carboxylate
4-[(3-Phenoxyphenyl)methyl]-1-piperazinecarboxylic acid 4-nitrophenyl ester
1-Piperazinecarboxylic acid, 4-[(3-phenoxyphenyl)methyl]-, 4-nitrophenyl ester
所屬類別
生物化工：激動(dòng)劑抑制劑物理化學(xué)性質(zhì)
沸點(diǎn)581.8±50.0 °C(Predicted)
密度1.303±0.06 g/cm3(Predicted)
儲存條件Sealed in dry,Store in freezer, under -20°C
溶解度加熱時(shí)在DMSO中的溶解度≥5mg/mL
酸度系數(shù)(pKa)6.13±0.10(Predicted)
形態(tài)粉末
顏色白色至米色
常見問題列表
生物活性
JZL195是有效的FAAH和MAGL抑制劑，IC50分別為2 nM和4 nM。靶點(diǎn)
| Target | Value |
|
FAAH
() | 2 nM |
|
MAGL
() | 4 nM |
體外研究
JZL195 produces near-complete blockade of FP-Rh labeling of both mouse brain FAAH and MAGL at concentrations as low as 100 nM (IC
50
values of 13 and 19 nM, respectively).
JZL195 inhibits rat and human FAAH and MAGL enzymes with IC
50
values in the range of ≈10-100 nM based on competitive ABPP assays.
體內(nèi)研究
JZL195 (20 mg/kg; i.p.) produces an antinociceptive response in the tail immersion assay.
| Animal Model: | Male C57BL/6J mice |
| Dosage: | 20 mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | Produced a much greater antinociceptive response in the tail immersion assay compared with inhibitors of either FAAH or MAGL alone. |