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Merck
모든 사진(1)

주요 문서

SML2793

Sigma-Aldrich

ZJ43

≥98% (HPLC)

동의어(들):

(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

실험식(Hill 표기법):
C12H20N2O7
CAS Number:
Molecular Weight:
304.30
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

분석

≥98% (HPLC)

양식

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

2-8°C

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

생화학적/생리학적 작용

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).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


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시험 성적서(COA)

Lot/Batch Number

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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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