His121 ARG57
- CAS No.
- 2135785-20-3
- Chemical Name:
- His121 ARG57
- Synonyms
- MAGL-IN-4;His121 ARG57;7-Oxa-5-azaspiro[3.4]octan-6-one, 2-[[3-[(3-chloro-4-methylphenyl)methoxy]-1-azetidinyl]carbonyl]-, cis-;Monoacylglycerol lipase,CB1,lipase,monoacylglycerol,CB2,Inhibitor,inhibit,BBB,barrier,MAGLIN4,MAGL IN 4,blood-brain,endocannabinoid,hERG,FAAH,2-AG,ABHD6,MAGL
- CBNumber:
- CB29731477
- Molecular Formula:
- C18H21ClN2O4
- Molecular Weight:
- 364.82
- MDL Number:
- MFCD34567353
- MOL File:
- 2135785-20-3.mol
His121 ARG57 Chemical Properties,Uses,Production
Biological Activity
MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain[1]. MAGL-IN-4 (compound 4f) shows a high LLE (5.9), a logD of 2.3 for MAGL[1]. MAGL-IN-4 exhibits no inhibition toward the closely related serine hydrolases (FAAH and ABHD6; all IC50>10000 nM). MAGL-IN-4 has no significant binding potentials to cannabinoid receptors (CB1: 19% and CB2: 5% at 10 μM), and low hERG liability (14.4% inh. at 10 μM, manual patch clamp, without BSA)[1]. MAGL-IN-4 (compound 4f; 0.1-10 mg/kg; oral; single dose) results in a significant elevation in the level of 2-AG and reduction in that of arachidonic acid (AA) from 0.3 mg/kg in C57BL/6J mice[1].
References
[1]. Shuhei Ikeda, et al. Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3-Oxo-3,4-dihydro-2 H-benzo[ b][1,4]oxazin-6-yl Moiety. J Med Chem. 2021 Aug 12;64(15):11014-11044.
His121 ARG57 Preparation Products And Raw materials
Raw materials
Preparation Products
His121 ARG57 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 | sales-cpd@caerulumpharma.com | China | 3423 | 58 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4153 | 55 | |
| DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9414 | 58 |
| Chunchuang (Wuhan) Technology Co., Ltd | 15342225168 | yutianchun2007@126.com | China | 10001 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24018 | 58 |
| Nantong QuanYi Biotechnology Co., Ltd | 0513-66337626 18051384581 | sales@chemhifuture.com | China | 4164 | 58 |
| Jiangsu Aikon Biopharmaceutical R&D co.,Ltd. | 025-66113011 18112977050 | cb5@aikonchem.com | China | 10529 | 58 |
| RD International Technology Co., Limited | 18024082417 | market@ubiochem.com | China | 9180 | 58 |