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ZJ43 | Potent inhibitor of glutamate carboxypeptidases II and III

ZJ43 (723331-20-2) is potent inhibitor of glutamate carboxypeptidases II (Ki = 0.8 nM) and III (Ki = 23 nM).1 It potently (IC50 = 2.4 nM) inhibited the ability of glutamate carboxypeptidase II to hydrolyze the neurotransmitter N-acetylaspartylglutamate (NAAG) resulting in an increase in synaptic levels of group II mGluRs. Peripherally administered ZJ43 increased the activation of mGluR3 by NAAG released from peripheral sensory neurites resulting in analgesia.2,3 ZJ43 has also shown efficacy in other inflammatory pain models.4,5

References/Citations
1) Olszewski et al. (2004), NAAG peptidase inhibition reduces locomotor activity and some stereotypes in the PCP model of schizophrenia via group II mGluR; J. Neurochem. 89 876
2) Yamamoto et al. (2004), Antinociceptive effects of N-acetylaspartylglutamate (NAAG) peptidase inhibitors ZJ-11, ZJ-17 and ZJ-43 in the rat formalin test and in the rat neuropathic pain model; Eur. J. Neurosci. 20 483
3) Yamamoto et al. (2007), Local administration of N-acetylaspartylglutamate (NAAG) peptidase inhibitors is analgesic in peripheral pain in rats; Eur. J. Neurosci. 25 147
4) Yamamoto et al. (2008), Intracerebroventricular administration of N-acetylaspartylglutamate (NAAG) peptidase inhibitors is analgesic in inflammatory pain; Mol. Pain 4 31
5) Nonaka et al. (2017), A role for the locus coeruleus in the analgesic efficacy of N-acetylaspartylglutamate peptidase (GCPII) inhibitors ZJ43 and 2-PMPA; Mol.Pain 13 1

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Catalog#  10-3904-0005

$95.00
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CAS:
723331-20-2
Catalog Number:
10-3904
Activity:
Potent inhibitor of glutamate carboxypeptidases II and III
Chemical Name:
N-[[[(1S)-1-Carboxy-3-methylbutyl]amino]carbonyl]-L-glutamic acid
Molecular Weight:
304.30
Molecular Formula:
C12H20N2O7
Solubility:
Soluble in DMSO (up to at least mg/ml) or in Water (up to at least 25 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or distilled water may be stored at -20° for up to 2 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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