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CP21 Sale

目录号 : GC48954

An iron chelator

CP21 Chemical Structure

Cas No.:30652-12-1

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产品描述

CP21 is an iron chelator that binds to iron in a 3:1 (ligand:iron) ratio.1 It is active against P. falciparum when used at concentrations of 10 and 100 µM.2 CP21 inhibits production of prostaglandin I2 induced by epinephrine, arachidonic acid , or A23187 in isolated rat aortic rings with IC50 values of 1.3, 1.3, and 1.4 mM, respectively.3 It inhibits glutamate-induced oxytosis, as well as decreases iodoacetic acid-induced cytotoxicity in an in vitro model of ischemia, in HT22 mouse hippocampal cells (EC50s = 13 and 9.5 µM, respectively).4 CP21 (200 mg/kg) increases the excretion of iron, but not copper, zinc, calcium, or magnesium, in rabbits.5

1.Dobbin, P.S., Hider, R.C., Hall, A.D., et al.Synthesis, physicochemical properties, and biological evaluation of N-substituted 2-alkyl-3-hydroxy-4(1H)-pyridinones: Orally active iron chelators with clinical potentialJ. Med. Chem.36(17)2448-2458(1993) 2.Heppner, D.G., Hallaway, P.E., Kontoghiorghes, G.J., et al.Antimalarial properties of orally active iron chelatorsBlood72(1)358-361(1988) 3.Jeremy, J.Y., Kontoghiorghes, G.J., Hoffbrand, A.V., et al.The iron chelators desferrioxamine and 1-alkyl-2-methyl-3-hydroxypyrid-4-ones inhibit vascular prostacyclin synthesis in vitroBiochem. J.254(1)239-244(1988) 4.Maher, P., and Kontoghiorghes, G.J.Characterization of the neuroprotective potential of derivatives of the iron chelating drug deferiproneNeurochem. Res.40(3)609-620(2015) 5.Kontoghiorghes, G.J., and Hoffbrand, A.V.Orally active α-ketohydroxy pyridine iron chelators intended for clinical use: In vivo studies in rabbitsBr. J. Haematol.62(4)607-613(1986)

Chemical Properties

Cas No. 30652-12-1 SDF
Canonical SMILES O=C1C=CN(CC)C(C)=C1O
分子式 C8H11NO2 分子量 153.2
溶解度 DMF: 1 mg/ml,DMSO: 1 mg/ml,Ethanol: 10 mg/ml,Ethanol:PBS (pH 7.2) (1:4): 0.20 mg/ml 储存条件 -20°C
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1 mM 6.5274 mL 32.6371 mL 65.2742 mL
5 mM 1.3055 mL 6.5274 mL 13.0548 mL
10 mM 0.6527 mL 3.2637 mL 6.5274 mL
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Research Update

Induction of immune responses in mice by a DNA vaccine encoding Cryptosporidium parvum Cp12 and CP21 and its effect against homologous oocyst challenge

Vet Parasitol 2010 Aug 27;172(1-2):1-7.PMID:20541869DOI:10.1016/j.vetpar.2010.04.036.

Cp12 and CP21 surface proteins on the sporozoite of Cryptosporidium parvum have been identified as the immunodominant antigens involved in the immune response to C. parvum infection. In the present study, the efficacy of Cp12 and CP21 antigens as vaccine candidates was investigated in BALB/c mice that were susceptible to C. parvum infection. DNA sequences of Cp12, CP21, Cp12-Cp21, and C (CpG oligodeoxynucleotide (ODN))-Cp12-Cp21 were amplified and then cloned into pVAX1 vector to form the four recombinant plasmids pVAX1-Cp12, pVAX1-Cp21, pVAX1-Cp12-Cp21, and pVAX1-C-Cp12-Cp21. Recombinant protein expression from these four plasmids in HeLa cells were confirmed by indirect immunofluorescence staining and Western blot analysis. The in vivo efficacies of the four DNA vaccines were tested in BALB/c mice. The results indicated that the four DNA vaccines elicited significant antibody responses and specific cellular responses when compared to control mice that received vector only or PBS. Among those four plasmids, pVAX1-C-Cp12-Cp21 elicited significantly higher levels of IgG. Also, the percentages of CD4(+) and CD8(+) T cells were significantly higher in the group with pVAX1-C-Cp12-Cp21 nasal sprays. Their efficacy in immunoprotection against homologous challenge was also detected after administration of the four DNA vaccines. The results showed that mice in the pVAX1-C-Cp12-Cp21 nasal group had a 77.5% reduction in the level of oocyst shedding and a significant difference was detected when this group was compared with the pVAX1, PBS, pVAX1-Cp12, and pVAX1-Cp21 groups. The reduction in the level of oocysts shedding from the group of pVAX1-C-Cp12-Cp21 nasal spray was also higher than that of pVAX1-Cp12-Cp21 group. These results suggested that C-Cp12-Cp21-DNA may provide an effective means of eliciting humoral and cellular responses and generating protective immunity against C. parvum infections in BALB/c mice.

The complete genome sequence of bacteriophage CP21 reveals modular shuffling in Campylobacter group II phages

J Virol 2012 Aug;86(16):8896.PMID:22843857DOI:10.1128/JVI.01252-12.

Campylobacter group II phages described so far share a high degree of sequence similarity. We report the 182,833-bp genomic sequence of the closely related group II phage CP21 and show that it has a completely different genomic organization. As in other group II phages, the CP21 genome is composed of large modules separated by long DNA repeat regions which obviously trigger recombination and modular shuffling.

Campylobacter group II phage CP21 is the prototype of a new subgroup revealing a distinct modular genome organization and host specificity

BMC Genomics 2015 Aug 22;16(1):629.PMID:26296758DOI:10.1186/s12864-015-1837-1.

Background: The application of phages is a promising tool to reduce the number of Campylobacter along the food chain. Besides the efficacy against a broad range of strains, phages have to be safe in terms of their genomes. Thus far, no genes with pathogenic potential (e.g., genes encoding virulence factors) have been detected in Campylobacter phages. However, preliminary studies suggested that the genomes of group II phages may be diverse and prone to genomic rearrangements. Results: We determined and analysed the genomic sequence (182,761 bp) of group II phage CP21 that is closely related to the already characterized group II phages CP220 and CPt10. The genomes of these phages are comprised of four modules separated by very similar repeat regions, some of which harbouring open reading frames (ORFs). Though, the arrangement of the modules and the location of some ORFs on the genomes are different in CP21 and in CP220/CPt10. In this work, a PCR system was established to study the modular genome organization of other group II phages demonstrating that they belong to different subgroups of the CP220-like virus genus, the prototypes of which are CP21 and CP220. The subgroups revealed different restriction patterns and, interestingly enough, also distinct host specificities, tail fiber proteins and tRNA genes. We additionally analysed the genome of group II phage vB_CcoM-IBB_35 (IBB_35) for which to date only five individual contigs could be determined. We show that the contigs represent modules linked by long repeat regions enclosing some yet not identified ORFs (e.g., for a head completion protein). The data suggest that IBB_35 is a member of the CP220 subgroup. Conclusion: Campylobacter group II phages are diverse regarding their genome organization. Since all hitherto characterized group II phages contain numerous genes for transposases and homing endonucleases as well as similar repeat regions, it cannot be excluded that these phages are genetically unstable. To answer this question, further experiments and sequencing of more group II phages should be performed.

Discovery of cellular substrates of human RNA-decapping enzyme DCP2 using a stapled bicyclic peptide inhibitor

Cell Chem Biol 2021 Apr 15;28(4):463-474.e7.PMID:33357462DOI:10.1016/j.chembiol.2020.12.003.

DCP2 is an RNA-decapping enzyme that controls the stability of human RNAs that encode factors functioning in transcription and the immune response. While >1,800 human DCP2 substrates have been identified, compensatory expression changes secondary to genetic ablation of DCP2 have complicated a complete mapping of its regulome. Cell-permeable, selective chemical inhibitors of DCP2 could provide a powerful tool to study DCP2 specificity. Here, we report phage display selection of CP21, a bicyclic peptide ligand to DCP2. CP21 has high affinity and selectivity for DCP2 and inhibits DCP2 decapping activity toward selected RNA substrates in human cells. CP21 increases formation of P-bodies, liquid condensates enriched in intermediates of RNA decay, in a manner that resembles the deletion or mutation of DCP2. We used CP21 to identify 76 previously unreported DCP2 substrates. This work demonstrates that DCP2 inhibition can complement genetic approaches to study RNA decay.

In vivo evaluation of hydroxypyridone iron chelators in a mouse model

Acta Haematol 1987;78(2-3):217-21.PMID:3120475DOI:10.1159/000205878.

The 59Fe excretion caused by a range of bidentate N-substituted [R group = methyl (CP20), ethyl (CP21), propyl (CP22), isopropyl (CP23), butyl (CP24) or hexyl (CP25)] 3-hydroxypyrid-4-one chelators in iron-overloaded mice is presented. All the compounds cause significant iron excretion when given intraperitoneally, but that the most hydrophobic compounds, CP24 and CP25, were toxic except at low doses. The excretion caused by CP21, CP22 and CP23 were significantly greater than that caused by CP20 and slightly larger than that caused by an equivalent dose of desferrioxamine. These compounds (CP20 through CP24) also caused significant excretion of 59Fe when administered orally. Compounds CP21, CP22 and CP24 were significantly more active than compounds CP20 and CP23. It is concluded that the N-ethyl or N-propyl 3-hydroxypyrid-4-ones are the most promising compounds for clinical application. Preliminary experiments using a hexadentate pyrid-2-one, CP130, show that this causes significant 59Fe excretion both when given intraperitoneally or orally.