Bioactivity | MAGL-IN-13 (compound (3R, 4S) - 5v) is a selective, irreversible inhibitor for MAGL,with IC50 values of 0.026, 0.021 and 0.24 nM for mMAGL, hMAGL and rMAGL, respectively. MAGL-IN-13 can penetrant blood brain barrier. [1]. |
Target | rats Ca2+ channel (10 μM) |
Invitro | MAGL-IN-13 (37 ℃预孵育 10 分钟)可以抑制mMAGL,hMACL 和 rMACL,IC50 值分别是0.026,0.021 和0.24 nM[1]。MAGL-IN-13 不可逆的抑制 MAGL 活性[1]。MAGL-IN-13(0.1 和 1 μM)对 MAGL 具有选择性[1]。MAGL-IN-13 在小鼠成纤维细胞 NIH3T3 中显示低细胞毒性,细胞活力的IC50值是 0.47 μM[1]。MAGL-IN-13 在10 μM 浓度下可以抑制大鼠的 Ca2+ 通道[1]。 0 --> MAGL-IN-13 相关抗体: Cell Cytotoxicity Assay[1] Cell Line: |
In Vivo | MAGL-IN-13(腹腔注射,5 mg/kg)抑制大脑 MAGL 的活性,具有剂量依赖性。 Animal Model: |
Name | MAGL-IN-13 |
Formula | C28H24FN5O4 |
Molar Mass | 513.52 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Butini S et al., Development of Potent and Selective Monoacylglycerol Lipase Inhibitors. SARs, Structural Analysis, and Biological Characterization. J Med Chem. 2024 Jan 19. doi: 10.1021/acs.jmedchem.3c01278. |