QNZ (EVP4593)

Modify Date: 2024-01-02 18:11:04

QNZ (EVP4593) Structure
QNZ (EVP4593) structure
Common Name QNZ (EVP4593)
CAS Number 545380-34-5 Molecular Weight 356.420
Density 1.3±0.1 g/cm3 Boiling Point 602.0±55.0 °C at 760 mmHg
Molecular Formula C22H20N4O Melting Point 169-175ºC
MSDS USA Flash Point 317.9±31.5 °C

 Use of QNZ (EVP4593)


QNZ shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC50s of 11 and 7 nM, respectively. EVP4593 is a neuroprotective inhibitor of SOC channel.

 Names

Name 4-N-[2-(4-phenoxyphenyl)ethyl]quinazoline-4,6-diamine
Synonym More Synonyms

 QNZ (EVP4593) Biological Activity

Description QNZ shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC50s of 11 and 7 nM, respectively. EVP4593 is a neuroprotective inhibitor of SOC channel.
Related Catalog
Target

NF-κB:11 nM (IC50, in human Jurkat cells transfected with pNFκB-Luc)

TNF-α:7 nM (IC50, in murine splenocytes stimulated with LPS)

In Vitro QNZ (Compound 11q) has a suppressing effect of the NF-κB mediated-inflammatory response. QNZ inhibits edema formation dose-dependently[1]. QNZ (EVP4593) reduces the number of lysosomes/autophagosomes and store-operated channel (SOC) currents in Huntington's disease (HD). Normalization of calcium transport within neurons in response to QNZ is expect to reduce pathology manifestation. A number of lysosomes/autophagosomes are evaluated in HD and WT neurons treated with QNZ using transmission electron microscopy (TEM). Incubation with QNZ reduces the number of lysosomes/autophagosomes in HD GABAergic medium spiny (GABA MS)-like neurons (GMSLNs) by almost two-fold (from 0.41±0.04 to 0.23±0.04; p<0.05), while WT neurons are not affected. This observation is confirmed by examining lysosome content by flow cytometry (FC) analysis. The median fluorescence intensity is reduced by 34±6 % in HD GMSLNs upon QNZ treatment (p<0.05)[2].
Cell Assay iPSHD22 cells are cultured in K-4 medium in a 96-well black plates with clear flat bottom. Next, cells are treated with chemical compounds (e.g., QNZ 100 nM) for 24 h prior to analysis. Fluorescent assay MultiTox-Fluor Multiplex Cytotoxicity Assay is used to measure simultaneously the relative number of live (viability) and dead (cytotoxicity) cells in each well. Fluorescence is detected by DTX 880 Multimode Microplate Reader. To evaluate the level of cell death (LoCD), the following equation is employed: ([cytotoxicity in a well with cells]-[cytotoxicity in a well without cells])/([viability in a well with cells]-[viability in a well without cells])[2].
References

[1]. Tobe M, et al. Discovery of quinazolines as a novel structural class of potent inhibitors of NF-kappa B activation.

[2]. Nekrasov ED, et al. Manifestation of Huntington's disease pathology in human induced pluripotent stem cell-derived neurons. Mol Neurodegener. 2016 Apr 14;11:27.

[3]. Wu J, et al. Enhanced Store-Operated Calcium Entry Leads to Striatal Synaptic Loss in a Huntington's Disease Mouse Model. J Neurosci. 2016 Jan 6;36(1):125-41.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 602.0±55.0 °C at 760 mmHg
Melting Point 169-175ºC
Molecular Formula C22H20N4O
Molecular Weight 356.420
Flash Point 317.9±31.5 °C
Exact Mass 356.163696
PSA 73.06000
LogP 4.57
Vapour Pressure 0.0±1.7 mmHg at 25°C
Index of Refraction 1.714
Storage condition Refrigerator, Under Inert Atmosphere
Water Solubility DMSO: soluble15mg/mL, clear

 Safety Information

RIDADR NONH for all modes of transport
HS Code 2933990090

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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 Synonyms

N-[2-(4-Phenoxyphenyl)ethyl]-4,6-quinazolinediamine
6-Amino-4-(4-phenoxyphenylethylamino)quinazoline
4,6-quinazolinediamine, N-[2-(4-phenoxyphenyl)ethyl]-
N-[2-(4-Phenoxyphenyl)ethyl]quinazoline-4,6-diamine
QNZ
NF-kappaB Activation Inhibitor
N4-[2-(4-Phenoxyphenyl)ethyl]-4,6-quinazolinediamine
EVP4593
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Price: $106/10mM*1mLinDMSO

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