NF 1819

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Cat.No. 5956 - NF 1819 | C24H22FN5O4 | CAS No. 1881244-28-5
Description: Potent and selective irreversible MAGL inhibitor; membrane permeable and brain penetrant
Chemical Name: (3R,4S)-rel-4-(1,3-Benzodioxol-5-yl)-3-(4-fluorophenyl)-1-[1-(1H)-1,2,4-triazol-1-carbonyl)-4-piperidinyl]-2-azetidinone
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent and selective irreversible MAGL inhibitor (IC50 values are 0.25 and 7.4 nM at rMAGL and hMAGL, respectively). Exhibits 389-fold selectivity over hFAAH and exhibits minimal binding at CB receptors (IC50 > 10 μM). Alleviates symptoms in a MS in vivo model. Exhibits analgesic effects in an acute inflammatory pain model in vivo. Ameliorates neuropathic hypersensitivity induced by oxaliplatin (Cat. No. 2623). Displays high membrane permeability and brain penetrant.

Technical Data

M. Wt 463.46
Formula C24H22FN5O4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1881244-28-5
Smiles FC1=CC=C([C@@H]2[C@@H](C3=CC=C4OCOC4=C3)N(C2=O)C5CCN(C(N6C=NC=N6)=O)CC5)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 46.35 100
ethanol 23.17 50

Preparing Stock Solutions

The following data is based on the product molecular weight 463.46. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.16 mL 10.79 mL 21.58 mL
5 mM 0.43 mL 2.16 mL 4.32 mL
10 mM 0.22 mL 1.08 mL 2.16 mL
50 mM 0.04 mL 0.22 mL 0.43 mL

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References

References are publications that support the biological activity of the product.

Brindisi et al (20106) Development and pharmacological characterization of selective blockers of 2-arachidonoyl glycerol degradation with efficacy in rodent models of multiple sclerosis and pain. J.Med.Chem. 59 2612 PMID: 26888301


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