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Home - Products - Metabolic Enzyme/Protease - Lipase - MAGL-IN-4

MAGL-IN-4

CAS No. 2135785-20-3

MAGL-IN-4( His121 ARG57 )

Catalog No. M28832 CAS No. 2135785-20-3

MAGL-IN-4 is one of the monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    MAGL-IN-4
  • Note
    Research use only, not for human use.
  • Brief Description
    MAGL-IN-4 is one of the monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases.
  • Description
    MAGL-IN-4 is one of the monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases.(In Vitro):MAGL-IN-4 showed potent in vitro MAGL inhibitory activity (IC50 6.2 nM), good oral absorption and blood-brain barrier penetration.(In Vivo):MAGL-IN-4 showed significant pharmacodynamic changes (2-arachidonoylglycerol increase and arachidonic acid decrease) at 0.3-10 mg/kg, po. in mice.
  • In Vitro
    MAGL-IN-4 (compound 4f) shows a high LLE (5.9), a logD of 2.3 for MAGL.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).
  • In Vivo
    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.
  • Synonyms
    His121 ARG57
  • Pathway
    Metabolic Enzyme/Protease
  • Target
    Lipase
  • Recptor
    ——
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2135785-20-3
  • Formula Weight
    364.82
  • Molecular Formula
    C18H21ClN2O4
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (274.11 mM)
  • SMILES
    O=C(OC1)N[C@@]21C[C@@H](C(N3CC(OCC4=CC=C(C)C(Cl)=C4)C3)=O)C2
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Jatczak, K., et al. Preparation of selectively protected protoescigenin derivatives for synthesis of escin analogs and neoglycoconjugates. cent.eur.j.chem. 12, 1222–1231 (2014).
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