KML29

SKU: orb1223324

Description

KML29 is highly selective and effective monoacylglycerol lipase (MAGL) inhibitor. It has effective inhibition of human/mouse/rat MAGL (IC50: 5.9/15/43 nM). It has not inhibitory for FAAH (IC50 > 50 μM). It also effectively and selectively blocks hydrolysis of 2-arachidonoylglycerol (2-AG) in mice (IC50: 2.5 nM, 2-AG; >50 μM, AEA).

Key Properties

• CAS Number: 1380424-42-9
• MW: 549.42
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₁F₆NO₇
• SMILES: O=C(OC(C(F)(F)F)C(F)(F)F)N1CCC(C(c2ccc3OCOc3c2)(O)c2cc3OCOc3cc2)CC1
• Target: GluR
• Solubility: DMSO : 50 mg/mL. 91.01 mM; H2O : < 0.1 mg/mL

Bioactivity

• In Vivo:
  KML29 enhibits antinociceptive activity without cannabimimetic side effects. KML29 (20 mg/kg) has a significant but modest protective effectagainst LPS-induced fever. Animal model: C57Bl/6 mice. Dosage: 1-40 mg/kg. Administration: p.o. single dose. Result: Selectively inhibited MAGL in mice. Animal model: Wistar albino male rats. Dosage: 20 mg/kg (+LPS E. coli O111: B4 (250 μg/kg, sc)). Administration: SC. Result: Administration of KML29 simultaneously with LPS E. coli O111: B4 significantly decreased T (with 5% type 1 error, 1.7 fold) compared to saline+LPS E. coli O111: B4. Administration of KML29 simultaneously with LPS E. coli O111: B4 resulted in decreased plateau phase of fever compared to LPS E. E. coli O111: B4+saline administration.
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• In Vitro:
  KML29 dose-dependently elevates brain 2-AG level up to10-fold without alteration in brain levels of anandamide, palmitoylethanolamide, and oleoylethanolamide. KML29 is a potent inhibitor of 2-AG hydrolysis, but did not affect AEA hydrolysis at any concentration tested.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

KML-29 | KML29 | KML 29

Quick Database Links

Gene Symbol

GluR