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Merck
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Documenti fondamentali

SML2793

Sigma-Aldrich

ZJ43

≥98% (HPLC)

Sinonimo/i:

(S)-2-(3-((S)-1-Carboxy-3-methylbutyl)ureido)pentanedioic acid, N-[[[(1S)-1-Carboxy-3-methylbutyl]amino]carbonyl]-L-glutamic acid, ZJ 43, ZJ-43

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About This Item

Formula empirica (notazione di Hill):
C12H20N2O7
Numero CAS:
Peso molecolare:
304.30
Numero MDL:
Codice UNSPSC:
12352200
NACRES:
NA.77

Livello qualitativo

Saggio

≥98% (HPLC)

Stato

powder

Colore

white to beige

Solubilità

DMSO: 2 mg/mL, clear

Temperatura di conservazione

2-8°C

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
BSGWCSGMXAVYRT-YUMQZZPRSA-N

Azioni biochim/fisiol

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).

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


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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
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
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
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:
Robert S Jansen et al.
The Journal of biological chemistry, 290(51), 30429-30440 (2015-10-31)
The ubiquitous efflux transporter ABCC5 (ATP-binding cassette subfamily C member 5) is present at high levels in the blood-brain barrier, neurons, and glia, but its in vivo substrates and function are not known. Using untargeted metabolomic screens, we show that

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