Ampalex - CAS 154235-83-3
Catalog number: 154235-83-3
Category: Inhibitor
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Molecular Formula:
C14H15N3O
Molecular Weight:
241.29
COA:
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Targets:
AMPAR
Description:
CX516 is a positive allosteric modulator at AMPA receptor that inhibits the deactivation of AMPA receptors. CX-516 is a nootropic and ampakine agent.
Purity:
>98%
Synonyms:
CX516; BDP 12; Ampakine CX516
MSDS:
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InChIKey:
ANDGGVOPIJEHOF-UHFFFAOYSA-N
InChI:
InChI=1S/C14H15N3O/c18-14(17-8-2-1-3-9-17)11-4-5-12-13(10-11)16-7-6-15-12/h4-7,10H,1-3,8-9H2
Canonical SMILES:
C1CCN(CC1)C(=O)C2=CC3=NC=CN=C3C=C2
1.Cytotoxic Potential of Bacillus cereus Strains ATCC 11778 and 14579 Against Human Lung Epithelial Cells Under Microaerobic Growth Conditions.
Kilcullen K1, Teunis A1, Popova TG1, Popov SG1. Front Microbiol. 2016 Feb 3;7:69. doi: 10.3389/fmicb.2016.00069. eCollection 2016.
Bacillus cereus, a food poisoning bacterium closely related to Bacillus anthracis, secretes a multitude of virulence factors including enterotoxins, hemolysins, and phospholipases. However, the majority of the in vitro experiments evaluating the cytotoxic potential of B. cereus were carried out in the conditions of aeration, and the impact of the oxygen limitation in conditions encountered by the microbe in natural environment such as gastrointestinal tract remains poorly understood. This research reports comparative analysis of ATCC strains 11778 (BC1) and 14579 (BC2) in aerobic and microaerobic (static) cultures with regard to their toxicity for human lung epithelial cells. We showed that BC1 increased its toxicity upon oxygen limitation while BC2 was highly cytotoxic in both growth conditions. The combined effect of the pore-forming, cholesterol-dependent hemolysin, cereolysin O (CLO), and metabolic product(s) such as succinate produced in microaerobic conditions provided substantial contribution to the toxicity of BC1 but not BC2 which relied mainly on other toxins.
2.Mechanism of oxidative conversion of Amplex® Red to resorufin: Pulse radiolysis and enzymatic studies.
Dębski D1, Smulik R1, Zielonka J2, Michałowski B1, Jakubowska M1, Dębowska K1, Adamus J1, Marcinek A1, Kalyanaraman B3, Sikora A4. Free Radic Biol Med. 2016 Mar 26;95:323-332. doi: 10.1016/j.freeradbiomed.2016.03.027. [Epub ahead of print]
Amplex® Red (10-acetyl-3,7-dihydroxyphenoxazine) is a fluorogenic probe widely used to detect and quantify hydrogen peroxide in biological systems. Detection of hydrogen peroxide is based on peroxidase-catalyzed oxidation of Amplex® Red to resorufin. In this study we investigated the mechanism of one-electron oxidation of Amplex® Red and we present the spectroscopic characterization of transient species formed upon the oxidation. Oxidation process has been studied by a pulse radiolysis technique with one-electron oxidants (N3•, CO3•-,•NO2 and GS•). The rate constants for the Amplex® Red oxidation by N3• (2k=2.1·109M-1s-1, at pH=7.2) and CO3•- (2k=7.6·108M-1s-1, at pH=10.3) were determined. Two intermediates formed during the conversion of Amplex® Red into resorufin have been characterized. Based on the results obtained, the mechanism of transformation of Amplex® Red into resorufin, involving disproportionation of the Amplex® Red-derived radical species, has been proposed.
3.Cascade DNA logic device programmed ratiometric DNA analysis and logic devices based on a fluorescent dual-signal probe of a G-quadruplex DNAzyme.
Fan D1, Zhu J1, Zhai Q1, Wang E1, Dong S1. Chem Commun (Camb). 2016 Feb 25;52(19):3766-9. doi: 10.1039/c5cc10556k.
Herein, two fluorescence sensitive substrates of G-quadruplex/hemin DNAzyme with inverse responses (Scopoletin and Amplex Red) were simultaneously used in one homogeneous system to construct a cascade advanced DNA logic device for the first time (a functional logic device (a three input based DNA calliper) cascade with an advanced non-arithmetic logic gate (1 to 2 decoder)). This cascade logic device was applied to label-free ratiometric target DNA detection and length measurement.
4.Tiered High-Throughput Screening Approach to Identify Thyroperoxidase Inhibitors Within the ToxCast Phase I and II Chemical Libraries.
Paul Friedman K1, Watt ED2, Hornung MW3, Hedge JM4, Judson RS5, Crofton KM5, Houck KA5, Simmons SO6. Toxicol Sci. 2016 Feb 15. pii: kfw034. [Epub ahead of print]
High-throughput screening for potential thyroid-disrupting chemicals requires a system of assays to capture multiple molecular-initiating events (MIEs) that converge on perturbed thyroid hormone (TH) homeostasis. Screening for MIEs specific to TH-disrupting pathways is limited in the U.S. Environmental Protection Agency ToxCast screening assay portfolio. To fill 1 critical screening gap, the Amplex UltraRed-thyroperoxidase (AUR-TPO) assay was developed to identify chemicals that inhibit TPO, as decreased TPO activity reduces TH synthesis. The ToxCast phase I and II chemical libraries, comprised of 1074 unique chemicals, were initially screened using a single, high concentration to identify potential TPO inhibitors. Chemicals positive in the single-concentration screen were retested in concentration-response. Due to high false-positive rates typically observed with loss-of-signal assays such as AUR-TPO, we also employed 2 additional assays in parallel to identify possible sources of nonspecific assay signal loss, enabling stratification of roughly 300 putative TPO inhibitors based upon selective AUR-TPO activity.
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