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ABX-1431

Cat. No. M13369
ABX-1431  Structure
Size Price Availability Quantity
10mg USD 83  USD83 In stock
25mg USD 162  USD162 In stock
50mg USD 270  USD270 In stock
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Quality Control & Documentation
Biological Activity

ABX-1431is a highly potent, selective and orally available CNS-osmotic monacylglycerol lipase (MAGL) inhibitor with IC50 values of 14 nM and 27 nM against human and mouse MGLL, respectively.

Chemical Information
Molecular Weight 507.39
Formula C20H22F9N3O2
CAS Number 1446817-84-0
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Lyndsey L Anderson, et al. Neuropharmacology. The endocannabinoid system impacts seizures in a mouse model of Dravet syndrome

[2] Kirsten R Mller-Vahl, et al. Mov Disord. Monoacylglycerol Lipase Inhibition in Tourette Syndrome: A 12-Week, Randomized, Controlled Study

[3] Hui Deng, et al. Acta Pharm Sin B. Monoacylglycerol lipase inhibitors: modulators for lipid metabolism in cancer malignancy, neurological and metabolic disorders

[4] Ming Jiang, et al. J Med Chem. Activity-Based Protein Profiling Delivers Selective Drug Candidate ABX-1431, a Monoacylglycerol Lipase Inhibitor, To Control Lipid Metabolism in Neurological Disorders

[5] Justin S Cisar, et al. J Med Chem. Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders

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Keywords: ABX-1431 supplier, MAGL, inhibitors, activators


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