Basic information Safety Supplier Related

ABX-1431

Basic information Safety Supplier Related

ABX-1431 Basic information

Product Name:
ABX-1431
Synonyms:
  • CS-2856
  • ABX1431;ABX 1431
  • ABX-1431
  • 1-Piperazinecarboxylic acid, 4-[[2-(1-pyrrolidinyl)-4-(trifluoromethyl)phenyl]methyl]-, 2,2,2-trifluoro-1-(trifluoromethyl)ethyl ester
  • 1,1,1,3,3,3-hexafluoropropan-2-yl 4-{[2-(pyrrolidin-1-yl)-4-(trifluoromethyl)phenyl]me thyl}piperazine-1-carboxylate
  • 1,1,1,3,3,3-Hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate
  • ABX-1431,inhibit,ABX 1431,Monoacylglycerol lipase,ABX1431,MAGL,Inhibitor
  • Elcubragistat
CAS:
1446817-84-0
MF:
C20H22F9N3O2
MW:
507.39
Mol File:
1446817-84-0.mol
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ABX-1431 Chemical Properties

storage temp. 
-20°C
solubility 
Soluble in DMSO (>25 mg/ml)
form 
solid
color 
White
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
InChI
InChI=1S/C20H22F9N3O2/c21-18(22,23)14-4-3-13(15(11-14)31-5-1-2-6-31)12-30-7-9-32(10-8-30)17(33)34-16(19(24,25)26)20(27,28)29/h3-4,11,16H,1-2,5-10,12H2
InChIKey
SQZJGTOZFRNWCX-UHFFFAOYSA-N
SMILES
N1(C(OC(C(F)(F)F)C(F)(F)F)=O)CCN(CC2=CC=C(C(F)(F)F)C=C2N2CCCC2)CC1
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ABX-1431 Usage And Synthesis

Description

ABX-1431 (1446817-84-0) is a potent (IC50 = 14 nM in vitro, 2.2 nM in human PC3 cells) and very selective (>100-fold over hABHD6, >200-fold over hPLA2G7) inhibitor of monoacylglycerol lipase (MAGL).1 Active in a rat formalin pain test at 3mg/kg. Orally bioavailable and CNS penetrant.

Uses

Elcubragistat (ABX-1431) is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.

in vivo

Elcubragistat (ABX-1431) inhibits MGLL activity in rodent brain (ED50=0.5-1.4 mg/kg), increases brain 2-AG concentrations, and suppresses pain behavior in the rat formalin pain model[1].

References

[1] JUSTIN S. CISAR. Identification of ABX-1431, a Selective Inhibitor of Monoacylglycerol Lipase and Clinical Candidate for Treatment of Neurological Disorders[J]. Journal of Medicinal Chemistry, 2018, 61 20: 9062-9084. DOI:10.1021/acs.jmedchem.8b00951

ABX-1431Supplier

Fujian boshi pharmaceutical technology co. LTD Gold
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ChemCell Biomedicine Co.,Ltd.
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020-13556033878 2965585218 13556033878
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BOC Sciences
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Shanghai Lollane Biological Technology Co.,Ltd.
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Shanghai Beckham Medical Technology Co., Ltd
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13816613772
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