產品描述: | JZL195 is a selective and efficacious dual fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) inhibitor with IC50s of 2 and 4 nM, respectively |
靶點: |
IC50: 2 nM (FAAH), 4 nM (MAGL);FAAH;?Lipase;?Autophagy |
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 (IC50 values of 13 and 19 nM, respectively). JZL195 inhibits rat and human FAAH and MAGL enzymes with IC50 values in the range of ≈10-100 nM based on competitive ABPP assays |
體內研究: |
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. |
參考文獻: |
1. Long JZ, et al. Dual blockade of FAAH and MAGL identifies behavioral processes regulated by endocannabinoid crosstalk in vivo. Proc Natl Acad Sci U S A. 2009 Dec 1;106(48):20270-5. 2. Anderson WB, et al. Actions of the dual FAAH/MAGL inhibitor JZL195 in a murine inflammatory pain model. Neuropharmacology. 2014 Jun;81:224-30. |
溶解性: |
soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.307 ml |
11.535 ml |
23.07 ml |
5 mM |
0.461 ml |
2.307 ml |
4.614 ml |
10 mM |
0.231 ml |
1.154 ml |
2.307 ml |
50 mM |
0.046 ml |
0.231 ml |
0.461 ml |
|
注意: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |