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关于此项目
经验公式(希尔记法):
C12H20N2O7
化学文摘社编号:
分子量:
304.30
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
SMILES string
N([C@@H](CC(C)C)C(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)O
InChI
1S/C12H20N2O7/c1-6(2)5-8(11(19)20)14-12(21)13-7(10(17)18)3-4-9(15)16/h6-8H,3-5H2,1-2H3,(H,15,16)(H,17,18)(H,19,20)(H2,13,14,21)/t7-,8-/m0/s1
InChI key
BSGWCSGMXAVYRT-YUMQZZPRSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Potent glutamate carboxypeptidase II (GCPII; NAAG peptidase; NAALADase I; PSMA) inhibitor that suppresses PCP-induced motor activity in vivo.
ZJ43 is a urea-based N-acetylaspartylglutamate (NAAG) analog and a potent glutamate carboxypeptidase II (GCPII; NAAG peptidase; N-acetylaspartylglutamate peptidase I; NAALADase I; prostate-specific membrane antigen; PSMA) inhibitor (Ki = 0.8 nM/hGCPII vs 23 nM/hGCPIII) with no affinity toward NMDAR or mGluRs. ZJ43 effectively suppresses phencyclidine-induced motor activity (150 mg ZJ43/kg, 10 mg PCP/kg i.p.) and displays antinociceptive efficacy (100 mg/kg i.v.) in rats in vivo. Comparing to Quisqualate and 2-PMPA, ZJ43 shows human species-selectivity over murine GCPII (Ki = 0.58 nM/h vs. 5.9 nM/m using respective avi-tagged extracellular GCPII).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Tatsuo Yamamoto et al.
The European journal of neuroscience, 20(2), 483-494 (2004-07-06)
The peptide neurotransmitter N-acetylaspartylglutamate (NAAG) acts as an agonist at group II metabotropic glutamate receptors (mGluRs). NAAG is inactivated by extracellular peptidase activity yielding glutamate and N-acetylaspartate. We recently developed a series of potent NAAG peptidase inhibitors, including ZJ-11, ZJ-17
[Insulin therapy today and tomorrow].
F Kuntschen
Revue medicale de la Suisse romande, 115(9), 713-716 (1995-09-01)
Chunlong Zhong et al.
Journal of neurotrauma, 22(2), 266-276 (2005-02-18)
Traumatic brain injury (TBI) produces a rapid and excessive elevation in extracellular glutamate associated with excitotoxicity and secondary brain pathology. The peptide neurotransmitter Nacetylaspartylglutamate (NAAG) suppresses glutamate transmission through selective activation of presynaptic Group II metabotropic glutamate receptor subtype 3
Sangeeta Ray Banerjee et al.
Bioconjugate chemistry, 27(6), 1447-1455 (2016-04-15)
(68)Ga-labeled, low-molecular-weight imaging agents that target the prostate-specific membrane antigen (PSMA) are increasingly used clinically to detect prostate and other cancers with positron emission tomography (PET). The goal of this study was to compare the pharmacokinetics of three PSMA-targeted radiotracers:
Ming Li et al.
Chemical science, 7(11), 6779-6785 (2017-04-30)
Precise visualization of tumor margins with characterization of microscopic tumor invasion are unmet needs in prostate oncology that demand approaches with high sensitivity and specificity. To address those needs we report surface-enhanced Raman scattering (SERS) based optical imaging for prostate
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