2. Metabolic Enzyme/Protease Neuronal Signaling GPCR/G Protein
  3. Aminopeptidase Carboxypeptidase mGluR
  4. ZJ43

ZJ43 is a NAAG peptidase inhibitor and glutamate carboxypeptidase II/III (GCP II/III) inhibitor with human GCP II IC50 of 2.4 nM and Ki of 0.8 nM. ZJ43 blocks N-acetylaspartylglutamate hydrolysis, elevates extracellular N-acetylaspartylglutamate levels, and activates group II metabotropic glutamate receptors (mGluR). ZJ43 can be used for the research of schizophrenia, inflammatory pain, neuropathic pain, and traumatic brain injury.

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ZJ43

ZJ43 Chemical Structure

CAS No. : 723331-20-2

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Description

ZJ43 is a NAAG peptidase inhibitor and glutamate carboxypeptidase II/III (GCP II/III) inhibitor with human GCP II IC50 of 2.4 nM and Ki of 0.8 nM. ZJ43 blocks N-acetylaspartylglutamate hydrolysis, elevates extracellular N-acetylaspartylglutamate levels, and activates group II metabotropic glutamate receptors (mGluR). ZJ43 can be used for the research of schizophrenia, inflammatory pain, neuropathic pain, and traumatic brain injury[1][2][3][4].

IC50 & Target[1]

group II mGlu receptors

 

In Vitro

ZJ43 (range sufficient to generate dose-response curves; 2 h) potently inhibits cloned human GCP II with a Ki of 0.8 nM[1].
ZJ43 (range sufficient to generate dose-response curves) inhibits cloned mouse GCP III with a Ki of 23 nM[1].
ZJ43 (2 h) inhibits cloned rat GCPII with a Ki of 3 nM[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

ZJ43 Related Antibodies
In Vivo

ZJ43 (150 mg/kg; i.p.; single dose) significantly reduces multiple PCP-induced schizophrenia-like behavioral symptoms in male Sprague-Dawley rats[1].
ZJ43 (10-100 mg/kg; i.v.; single dose) produces dose-dependent analgesia in the rat Formalin inflammatory pain model[3].
ZJ43 (10-100 mg/kg; i.v.; single dose) produces dose-dependent antiallodynic effects in the rat partial sciatic nerve ligation neuropathic pain model[3].
ZJ43 (100 mg/kg; i.v.; single dose) does not alter acute nociceptive responses to noxious mechanical or thermal stimulation in healthy rats[3].
ZJ43 (50-150 mg/kg; i.p.; every 8 h; 3 total doses) significantly reduces ipsilateral neuronal degeneration in rat lateral fluid percussion TBI[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (male, 280-330 g, PCP-induced schizophrenia-like symptoms)[1]
Dosage: 150 mg/kg
Administration: i.p.; single dose
Result: Significantly reduced PCP-induced motor activity, with a statistically significant difference in total distance traveled between 80-180 min compared to PCP-only treated rats (p = 0.021).
Significantly increased the frequency of rats being "still" (p = 0.015).
Significantly reduced PCP-induced stereotypic falling (p = 0.02), circling movements (p ≤ 0.001), total head movements (p = 0.005), and head bobbing (p = 0.004) compared to PCP-only treated rats.
Produced a non-statistically significant trend toward reduced PCP-induced mouth movements, tremors, and sideways head movements.
Failed to reduce PCP-induced sniffing and showed a non-significant tendency to increase this behavior (p = 0.17).
Animal Model: Rats (Formalin-induced inflammatory pain model)[3]
Dosage: 10 mg/kg; 100 mg/kg
Administration: i.v.; single dose
Result: Decreased cumulative formalin-evoked flinches in both phase 1 (0-6 minutes) and phase 2 (10-60 minutes) in a dose-dependent manner (phase 1 P < 0.005, phase 2 P < 0.001).
Reduced flinching to ~50% of vehicle response in phase 1 and ~30% of vehicle response in phase 2 at 100 mg/kg.
Animal Model: Rats (partial sciatic nerve ligation neuropathic pain model)[3]
Dosage: 10 mg/kg; 100 mg/kg
Administration: i.v.; single dose
Result: Significantly increased the maximum 50% probability mechanical withdrawal threshold in a dose-dependent manner (P < 0.001).
Elevated the threshold to ~13 g at 100 mg/kg (compared to ~2 g in saline-treated rats).
Animal Model: Rats[3]
Dosage: 100 mg/kg
Administration: i.v.; single dose
Result: Had no significant effect on the number of paw withdrawal responses to noxious mechanical stimulation, with maximum responses (18.8) and minimum responses (15.6) not differing significantly from saline-treated rats (P > 0.3).
Had no significant effect on hotplate response latency, with % maximum possible effect (-9.9) not differing significantly from saline-treated rats (P > 0.8).
Animal Model: Sprague-Dawley (male, 340 g, lateral fluid percussion TBI moel)[4]
Dosage: 50 mg/kg; 100 mg/kg; 150 mg/kg
Administration: i.p.; every 8 h; 3 total doses
Result: Significantly reduced the number of ipsilateral degenerating neurons in the hippocampal CA2/3 regions compared to vehicle (p < 0.01).
Reduced ipsilateral astrocyte loss to 14.0% versus 30.6% in the vehicle group at 50 mg/kg dose (p = 0.05; p = 0.007).
Molecular Weight

304.30

Formula

C12H20N2O7
CAS No.
Appearance

Solid

Color

Colorless to off-white

SMILES

O=C(N[C@H](C(O)=O)CCC(O)=O)N[C@H](C(O)=O)CC(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: 99.6%

SDS (393 KB)

COA (248 KB)

Handling Instructions (2659 KB)
References
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ZJ43 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ZJ43723331-20-2ZJ 43ZJ-43AminopeptidaseCarboxypeptidasemGluRMetabotropic glutamate receptorsN-acetylaspartylglutamatemale Sprague-Dawley ratsgroup II metabotropic glutamate receptorsinflammatory painNMDA receptorglutamate carboxypeptidase IIIrat cerebellar granule cellsglutamate carboxypeptidase IItraumatic brain injuryneuropathic painInhibitorinhibitorinhibit

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