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
Size Price / USD Stock Quantity
5MG 356 Get Quote
10MG 530 Get Quote
25MG 851 Get Quote
50MG 1152 Get Quote
100MG 1557 Get Quote
500MG 3114 Get Quote
1G Get Quote Get Quote

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).
molnova catalog
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