| Identification | Back Directory | [Name]
JJKK 048 | [CAS]
1515855-97-6 | [Synonyms]
JJKK 048
JJKK-048 >=98% (HPLC)
4-[Bis(1,3-benzodioxol-5-yl)methyl]-1-piperidinyl]-1H-1,2,4-triazol-1-yl-methanone
Methanone, [4-[bis(1,3-benzodioxol-5-yl)methyl]-1-piperidinyl]-1H-1,2,4-triazol-1-yl- | [Molecular Formula]
C23H22N4O5 | [MOL File]
1515855-97-6.mol | [Molecular Weight]
434.44 |
| Chemical Properties | Back Directory | [Boiling point ]
615.9±65.0 °C(Predicted) | [density ]
1.52±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble to 100 mM in DMSO | [form ]
Powder | [pka]
1.70±0.10(Predicted) | [color ]
White to off-white | [InChI]
1S/C23H22N4O5/c28-23(27-12-24-11-25-27)26-7-5-15(6-8-26)22(16-1-3-18-20(9-16)31-13-29-18)17-2-4-19-21(10-17)32-14-30-19/h1-4,9-12,15,22H,5-8,13-14H2 | [InChIKey]
CLSNATLUIXZPMV-UHFFFAOYSA-N | [SMILES]
O=C(N1N=CN=C1)N2CCC(C(C3=CC(OCO4)=C4C=C3)C5=CC=C(OCO6)C6=C5)CC2 |
| Hazard Information | Back Directory | [Uses]
JJKK 048 inhibits monoacylglycerol lipase by terminating signaling pathway of 2-arachidonoylglycerol in mouse brain and human melanoma cell proteome. JJKK 048 can be classified as a MAGL inhibitor that has therapeutic potential for the treatment of cancers. | [Biological Activity]
JJKK-048 is a cell penetrant ultrapotent and highly selective inhibitor of monoacylglycerol lipase (MAGL) th at exhibits a low cross-reactivity with other endocannabinoid targets. JJKK-048 is an irreversible inhibitor th at binds to the active site S122. | [in vivo]
JJKK 048 (0.1-4 mg/kg; i.p.; single dose; acute administration) potently inhibits MAGL and elevates brain 2-Arachidonoylglycerol (2-AG) (HY-W011051) levels in male C57Bl/6J mice[2].
JJKK 048 (0.5-2 mg/kg; i.p.; single dose; acute administration) inhibits MAGL in peripheral tissues (liver, spleen, heart, and skeletal muscle) with some off - target effects in mouse[2].
JJKK 048 (0.5 mg/kg; i.p.; single dose; acute administration) promotes significant analgesia in a writhing test in male Albino Swiss mice without causing cannabimimetic side effects[2].
JJKK 048 (1-2 mg/kg; i.p.; single dose; acute administration) induces analgesia both in the writhing test and in the tail - immersion test, as well as hypomotility and hyperthermia, but not catalepsy in male Albino Swiss mice[2].
| Animal Model: | Male C57Bl/6J mice (8 weeks old, weight 20-26 g)[2] | | Dosage: | 0.1 mg/kg, 0.5 mg/kg, 1 mg/kg, 2 mg/kg, 4 mg/kg, (dissolved in 5% (v/v) dimethylsulfoxide (DMSO) in gently heated 10% (w/v) HP-β-CD (HY-101103)) | | Administration: | i.p., single dose | | Result: | Revealed a dose-dependent blockade of MAGL in the brain.
Increased brain 2-AG levels in a dose-dependent manner, while brain AEA levels remained unaffected. |
| Animal Model: | Male Albino Swiss mice (weight 20-30 g), tetrad test model for cannabimimetic effects[2] | | Dosage: | 0.5 mg/kg, 1 mg/kg, 2 mg/kg (dissolved in 5% (v/v) DMSO in gently heated 10% (w/v) HP-β-CD (HY-101103)) | | Administration: | i.p., single dose | | Result: | Caused significant reduction in the writhing episodes of mice in the writhing test, indicating an antinociceptive effect. |
| [storage]
Store at -20°C |
|
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|