magl-in-1

MAGL-IN-1 is a selective and potent monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 80 nM.

FAAH MAGL-IN-1, also known as compound SIH 3, is a highly effective inhibitor of FAAH (fatty acid amide hydrolase) and MAGL (monoacylglycerol lipase). It exhibits IC50 values of 31 nM and 29 nM against FAAH and MAGL, respectively. This compound shows promising potential for advancing research in the field of neuropathic pain [1].

MAGL-IN-14 (compound 2) 作为一种高效的MAGL抑制剂，展现出了卓越的生物活性，其在HEK293和PC3细胞系中的IC50值分别达到了0.00289 μM和0.002 μM。

MAGL-IN-10为一种可逆MAGL抑制剂，展现出优良的ADME特性且体内毒性低。该化合物适用于癌症、神经系统疾病和炎症病理学研究。

MAGL-IN-11（化合物 29），一种选择性且可逆的MAGL抑制剂，具备研究炎症、癌症和抗氧化潜力。

MAGL-IN-15 (Compound 6) 为MAGL抑制剂，用于研究与内大麻素系统信号活动调节相关的疾病和病症。

MAGL-IN-18 (compound 118) 作为一种高效的单酰基甘油脂肪酶(MAGL)抑制剂，具有0.03nM的IC50值。

MAGL-IN-19 (compound 7o) 表现出高度的效力与选择性，作为MAGL的抑制剂。

OMDM169 is a potent and selective MAGL inhibitor. OMDM169 could enhances 2-AG levels and of exerts analgesic activity via indirect activation of cannabinoid receptors. OMDM169 exhibited 0.13 microMing activities in

MAGL-IN-9 (compound 16)为高选择性、可逆MAGL抑制剂，其IC50值为2.7 nM[1]< sup >。

URB754 is a potent and noncompetitive inhibitor of monoacylglycerol lipase (MAGL), exhibiting an IC50 value of 200 nM for the recombinant rat brain enzyme. However, it does not inhibit human recombinant, rat brain, or mouse brain MAGL at concentrations up to 100 μM. There is evidence that the MAGL inhibitory activity of URB754 may be attributed to the impurity bis(methylthio)mercurane (IC50 = 11.9 nM for rat recombinant MAGL) that is found in commercial preparations. URB754 inhibits rat brain fatty acyl amide hydrolase (FAAH) with an IC50 value of 32 μM and binds weakly to the rat central cannabinoid (CB1) receptor with an IC50 value of 3.8 μM. It does not inhibit COX-1 or COX-2 at concentrations up to 100 μM. Inhibition of MAGL hydrolysis of 2-arachidonoyl glycerol (2-AG) is associated with enhanced stress-induced analgesia and may represent a novel drug target in pain and stress management.

MAGL-IN-8 (compound 13) 是一种针对 hMAGL 的高选择性可逆抑制剂，其IC50值为2.5 ± 0.4 nM。

CAY10762 is an inhibitor of monoacylglycerol lipase (MAGL; IC50= 34.1 nM).1It reduces hydrogen peroxide-induced lactate dehydrogenase (LDH) release from Neuro2a cells when used at a concentration of 1 μM. CAY10762 (10 mg kg) increases levels of 2-arachidonoyl glycerol in mouse brain. 1.Castelli, R., Scalvini, L., Vacondio, F., et al.Benzisothiazolinone derivatives as potent allosteric monoacylglycerol lipase inhibitors that functionally mimic sulfenylation of regulatory cysteinesJ. Med. Chem.63(3)1261-1280(2020)

FAAH MAGL-IN-2 是一种有效的，可逆的，具有口服活性且可透过血脑屏障的 FAAH 和 MAGL 抑制剂，其IC50值分别为 11 nM 和 36 nM (b>Ki 值分别为 28 nM 和 60 nM)。FAAH MAGL-IN-2 有研究神经性疼痛的潜力而不引起运动障碍。