Tag: 200-300

《Cu-Catalyzed site-selective C(sp2)-H radical trifluoromethylation of tryptophan-containing peptides》 was written by Guerrero, Itziar; Correa, Arkaitz. Computed Properties of C12H15ClN2O2This research focused ontryptophan peptide radical trifluoromethylation copper catalyst chirality; crystal structure tryptophan trifluoromethylation reaction mechanism solvent effect. The article conveys some information:

Site-selective functionalization of C-H bonds within a peptide framework poses a challenging task of paramount synthetic relevance. Herein, we report an operationally simple C(sp2)-H trifluoromethylation of tryptophan (Trp)-containing peptides. This fluorination technique is characterized by its chirality preservation, tolerance of functional groups, and scalability and exhibits chemoselectivity for Trp residues over other amino acid and heterocyclic units. As a result, it represents a sustainable tool toward the late-stage peptide modification and protein engineering.H-Trp-OMe.HCl(cas: 7524-52-9Computed Properties of C12H15ClN2O2) was used in this study.

H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.Computed Properties of C12H15ClN2O2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

《C-H olefination of tryptophan residues in peptides: Control of residue selectivity and peptide-amino acid cross-linking》 was written by Terrey, Myles J.; Holmes, Ashley; Perry, Carole C.; Cross, Warren B.. Category: esters-buliding-blocksThis research focused ontryptophan peptide synthesis olefination solvent effect; peptide amino acid cross linking residue selectivity; protective group peptide coupling. The article conveys some information:

There is high demand for new methods to modify peptides, for application in drug discovery and biomedicine. A C-H functionalization protocol for the olefination of tryptophan residues in peptides is described. The modification is successful for Trp residues at any position in the peptide, has broad scope in the styrene coupling partner, and offers opportunities for conjugating peptides with other biomols. For peptides containing both Trp and Phe, directing group manipulation enables full control of residue selectivity. In the experiment, the researchers used H-Trp-OMe.HCl(cas: 7524-52-9Category: esters-buliding-blocks)

H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.Category: esters-buliding-blocks

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Formula: C11H24N2O2In 2020 ,《Impact of amino acids on the aqueous self-assembly of benzene trispeptides into supramolecular polymer bottle brushes》 was published in Polymer Chemistry. The article was written by Klein, Tobias; Ulrich, Hans F.; Gruschwitz, Franka V.; Kuchenbrod, Maren T.; Takahashi, Rintaro; Fujii, Shota; Hoeppener, Stephanie; Nischang, Ivo; Sakurai, Kazuo; Brendel, Johannes C.. The article contains the following contents:

In contrast to covalent polymer brushes, directional supramol. forces such as hydrogen bonds or π-π-interactions govern the formation of supramol. polymer bottle brushes (SPBs) in a self-assembly process starting from single polymer building units. In an attempt to broaden our understanding of these processes and the required supramol. forces, we here investigated the benzene trispeptide (BTP) motif to self-assemble polyethylene oxide (PEO) chains into SPBs in water. For this purpose, we synthesized a library of BTP-PEO conjugates, in which we varied the amino acid unit (alanine vs. leucine vs. phenylalanine), the hydrophobic spacer (C6 vs.C12), and the steric hindrance imposed by PEO (2 vs. 5 vs. 10 kg mol-1, one vs. three polymer chains). In particular, the type of amino acid was hypothesized to have a crucial influence on the final morphol. A detailed characterization of the resp. solutions revealed that for the C6 spacer and one PEO2k chain, only phenylalanine containing core units formed the desirable SPBs, while in the other cases only spherical micelles (leucine) or barely any aggregation (alanine) was observed In contrast, the more hydrophobic C12 spacer resulted in an exclusive formation of SPBs, whereas the choice of the amino acid moiety had a minor influence on the observed morphol. Increasing the steric hindrance finally resulted in a transition from cylindrical toward spherical micelles. The broad structural variety offered by the choice of amino acids not only allows for an excellent control of the solution morphologies but also the potential integration of functional units to the core. In the experiment, the researchers used N-Boc-1,6-Diaminohexane(cas: 51857-17-1Formula: C11H24N2O2)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is used to prepare 1,3-Bis[6-(Boc-amino)hexyl]urea by reacting with carbonyl dichloride in the presence of triethylamine. Further, it is used as a reagent for the introduction of a C6-spacer.Formula: C11H24N2O2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Recommanded Product: tert-Butyl (5-aminopentyl)carbamateIn 2019 ,《Pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines to develop functionalized ligands to target adenosine receptors: Fluorescent ligands as an example》 appeared in MedChemComm. The author of the article were Federico, Stephanie; Margiotta, Enrico; Paoletta, Silvia; Kachler, Sonja; Klotz, Karl-Norbert; Jacobson, Kenneth A.; Pastorin, Giorgia; Moro, Stefano; Spalluto, Giampiero. The article conveys some information:

A series of adenosine receptor antagonists bearing a reactive linker was developed. Functionalization of these derivatives is useful to easily obtain multi-target ligands, receptor probes, drug delivery systems, and diagnostic or theranostic systems. The pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines scaffold was chosen as a pharmacophore for the adenosine receptors. It was substituted at the 5-position with reactive linkers of different lengths. Then, these compounds, e.g., I, were used to synthesize probes for the adenosine receptors by functionalization with a fluorescent moiety. Both series of compounds were evaluated for their binding at the four adenosine receptor subtypes. Different affinity and selectivity profiles were observed towards hA1, hA2A and hA3 adenosine receptors. In particular, fluorescent compounds II [R = -(CH2)3-, -(CH2)5-, -(CH2)2O(CH2)2O(CH2)2-, etc.] behave as dual hA2A/hA3 ligands. Computational studies suggested different binding modes for developed compounds at the three receptors. Both mol. docking and supervised mol. dynamics (SuMD) simulations confirmed that the preferred binding mode at the single receptor was driven by the substitution present at the 5-position. The obtained results rationalized the compounds’ binding profile at the adenosine receptors and pave the way for the development of more potent conjugable and conjugated ligands targeting these membrane receptors. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Recommanded Product: tert-Butyl (5-aminopentyl)carbamate)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Recommanded Product: tert-Butyl (5-aminopentyl)carbamate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Quality Control of tert-Butyl (5-aminopentyl)carbamateIn 2021 ,《In vitro and in vivo degradation of programmed cell death ligand 1 (PD-L1) by a proteolysis targeting chimera (PROTAC)》 appeared in Bioorganic Chemistry. The author of the article were Wang, Yubo; Zhou, Yuanyuan; Cao, Sheng; Sun, Yue; Dong, Zhiqiang; Li, Chen; Wang, Haoran; Yao, Yuhong; Yu, Haiyan; Song, Xiangyi; Li, Ming; Wang, Jiefu; Wei, Mingming; Yang, Guang; Yang, Cheng. The article conveys some information:

Immunotherapy via immune checkpoints blockade has aroused the attention of researchers worldwide. Inhibition of the programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction has been one of the most promising immunotherapy strategies. Several neutralizing antibodies targeting this interaction have been developed, which have already achieved considerable clin. success. Addnl., numerous pharmaceutical companies have been committed to develop small mols. which could block the interaction between PD-1 and PD-L1. In this study, a novel PROTAC mol. 21a was developed, and effectively induced the degradation of PD-L1 protein in various malignant cells in a proteasome-dependent manner. Moreover, compound 21a could significantly reduce PD-L1 protein levels of MC-38 cancer cells in vivo, by which promoted the invasion of CD8+ T cells and inhibited the growth of MC-38 in vivo. This PROTAC mol. could be used as a novel and alternative strategy for cancer immunotherapy. In the experiment, the researchers used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Quality Control of tert-Butyl (5-aminopentyl)carbamate)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Quality Control of tert-Butyl (5-aminopentyl)carbamate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2022,Li, Yachao; Shen, Cheng; Liang, Xiaoyu; Deng, Kefurong; Zeng, Zenan; Xu, Xianghui published an article in Biomaterials Science. The title of the article was 《Dynamic-responsive virus-mimetic nanocapsules facilitate protein drug penetration and extracellular-specific unpacking for antitumor treatment》.Recommanded Product: 51857-17-1 The author mentioned the following in the article:

Protein-based drugs have been demonstrating great potential for the treatment of various diseases, but most of them encounter many difficulties in clin. trials or uses, such as instability, low bioavailability, and poor in vivo efficacy. In this work, we developed virus-mimetic nanocapsules (VMNs) for improving protein systemic delivery and pharmaceutical effects through bioinspired macromol. and supramol. engineering. These VMNs possessed hierarchical nanostructures including artificial capsids, encapsulated proteins, and synthetic envelopes. These dynamic-responsive VMNs can harbor protein drugs, resist protein adsorption, target solid tumors, penetrate into deep tissue, and site-specifically unpack protein drugs. Through surmounting the sequential physio-pathol. barriers, protein-loaded VMNs successfully maximized the in vitro and in vivo therapeutic efficacy of proteins, giving a promising strategy to address dilemmas on clin. TRAIL therapy. This study is expected to promote in vivo treatment outcomes and clin. transformation of protein drugs. In addition to this study using N-Boc-1,6-Diaminohexane, there are many other studies that have used N-Boc-1,6-Diaminohexane(cas: 51857-17-1Recommanded Product: 51857-17-1) was used in this study.

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) can be used as a linear hexyl spacer (C6-spacer) to synthesize biodegradable poly(disulfide amine)s for gene delivery, a multifunctional dendrimer for theranostics and so on.Recommanded Product: 51857-17-1

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

《Integration of [12]aneN3 and Acenaphtho[1,2-b]quinoxaline as non-viral gene vectors with two-photon property for enhanced DNA/siRNA delivery and bioimagingã€?was written by Liu, Jin-Yu; Liu, Xu-Ying; Liu, Rui; Tang, Fang; Yang, Jing-Bo; Tang, Quan; Lu, Zhong-Lin; Qiao, Hai-Jun; He, Lan. Recommanded Product: N-Boc-1,6-Diaminohexane And the article was included in Bioorganic Chemistry in 2021. The article conveys some information:

Two-photon fluorescent Acenaphtho[1,2-b]quinoxaline (ANQ) and the hydrophilic di-(triazole-[12]aneN3) moieties were combined through an alkyl chain (ANQ-A-M) or a β-hairpin motif with two aromatic γ-amino acid residues (ANQ-H-M) to explore their capabilities for in vitro and in vivo gene delivery and tracing. ANQ-A-M and ANQ-H-M showed the same maximum absorption at 420 nm, and their fluorescent intensities around 650 nm were varied in different solvents and became poor in the protic solvents. Gel electrophoresis assays indicated that both compounds completely retarded the migration of pDNA at 20 μM in the presence of DOPE. However, the DNA condensation with ANQ-H-M was not reversible, and the particle size of the corresponding complexes were larger indicated from the SEM and DLS measurements. In vitro transfections indicated ANQ-A-M/DOPE achieved Luciferase and GFP expressions were to be 7.9- and 5.7-fold of those by Lipo2000 in A549 cells resp. However, ANQ-H-M showed very poor transfection efficiency in Luciferase expression. With the help of single/two-photon fluorescence imaging it clearly demonstrated that the successful transfection of ANQ-A-M was attributed to its cellular uptake, apparent lysosomal escape, and reversible release of DNA; and the poor transfection of ANQ-H-M was resulted from the aggregation of the DNA complexes which prevented them from the cellular uptake, and also the strong binding ability which is not easy to release DNA. ANQ-A-M/DOPE also exhibited robust gene silencing (83% knockdown of Luciferase) and GFP expression (2.47-fold higher) efficiency compared with Lipo2000 in A549 and zebrafish, resp. The work demonstrated that the linkage structure between fluorescent and di(triazole-[12]aneN3) played the important role for their gene delivery performance, and that ANQ-A-M represents a vector with the strong transfection efficiency in vitro and in vivo as well as the efficient real time bioimaging properties, which is potential for the development in biomedical research. In the experiment, the researchers used many compounds, for example, N-Boc-1,6-Diaminohexane(cas: 51857-17-1Recommanded Product: N-Boc-1,6-Diaminohexane)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) can be used as a linear hexyl spacer (C6-spacer) to synthesize biodegradable poly(disulfide amine)s for gene delivery, a multifunctional dendrimer for theranostics and so on.Recommanded Product: N-Boc-1,6-Diaminohexane

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2016,Sellars, Jonathan D.; Skipsey, Mark; Sadr-ul-Shaheed; Gravell, Sebastian; Abumansour, Hamza; Kashtl, Ghasaq; Irfan, Jawaria; Khot, Mohamed; Pors, Klaus; Patterson, Laurence H.; Sutton, Chris W. published 《Rational Development of Novel Activity Probes for the Analysis of Human Cytochromes P450ã€?ChemMedChem published the findings.Synthetic Route of C10H22N2O2 The information in the text is summarized as follows:

The identification and quantification of functional cytochromes P 450 (CYPs) in biol. samples is proving important for robust analyses of drug efficacy and metabolic disposition. A novel CYP activity-based probe was rationally designed and synthesized, demonstrating selective binding of CYP isoforms. The dependence of probe binding upon the presence of NADPH permits the selective detection of functionally active CYP. This allows the detection and anal. of these enzymes using biochem. and proteomic methodologies and approaches. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Synthetic Route of C10H22N2O2)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Synthetic Route of C10H22N2O2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

《Photochemical chemoselective alkylation of tryptophan-containing peptidesã€?was written by Laroche, Benjamin; Tang, Xinjun; Archer, Gaetan; Di Sanza, Riccardo; Melchiorre, Paolo. HPLC of Formula: 7524-52-9This research focused ontryptophan peptide photochem chemoselective alkylation light radical precursor; peptide coupling alkylation mechanism enantioselective diastereoselective synthesis. The article conveys some information:

We report a photochem. method for the chemoselective radical functionalization of tryptophan (Trp)-containing peptides. The method exploits the photoactivity of an electron donor-acceptor complex generated between the tryptophan unit and pyridinium salts. Irradiation with weak light (390 nm) generates radical intermediates right next to the targeted Trp amino acid, facilitating a proximity-driven radical functionalization. This protocol exhibits high chemoselectivity for Trp residues over other amino acids and tolerates biocompatible conditions. In addition to this study using H-Trp-OMe.HCl, there are many other studies that have used H-Trp-OMe.HCl(cas: 7524-52-9HPLC of Formula: 7524-52-9) was used in this study.

H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.HPLC of Formula: 7524-52-9

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Product Details of 51857-17-1In 2022 ,《Synthesis of novel reactive disperse dyes comprising carbamate and cyanuric chloride groups for dyeing polyamide and cotton fabrics in supercritical carbon dioxideã€?appeared in Dyes and Pigments. The author of the article were Penthala, Raju; Oh, Hyeon; Park, Si Hyeong; Lee, In Yeol; Ko, Eun Hee; Son, Young-A.. The article conveys some information:

Two types of novel reactive disperse dyes comprising carbamates (CNU-6A, CNU-6B and CNU-6C) and cyanuric chloride (CNU-8A, CNU-8B and CNU-8C) reactive functional groups were designed and synthesized from the anthraquinone parent body. The structures of these synthesized reactive disperse dyes have been defined by IR, 1H NMR, 13C NMR, HRMS and UV-Vis spectroscopy. Further, the dyeing experiments were performed on polyamide and cotton fabrics in supercritical carbon dioxide conditions with the 0.5% (owf) of dye concentration, at 25 MPa (pressure), and 120°C (temperature) for 1 h. A significant improvement in the color strength and dye fixation efficiency has been observed for the carbamate reactive disperse dyes. This is due to the formation of a covalent bond between the carbamate functional group and the amine (-NH) and hydroxy (-OH) group of the fabrics. Besides, the dyed fabrics displayed favorable fastness (wash, crocking, light and sweat) properties indicating that the synthesized dyes meet the garment dyeing standards In the experimental materials used by the author, we found N-Boc-1,6-Diaminohexane(cas: 51857-17-1Product Details of 51857-17-1)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is used to prepare 1,3-Bis[6-(Boc-amino)hexyl]urea by reacting with carbonyl dichloride in the presence of triethylamine. Further, it is used as a reagent for the introduction of a C6-spacer.Product Details of 51857-17-1

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics