Tag: 200-300

Martinson, Elizabeth A.; Scheible, Stephan; Presek, Peter published an article in Cellular and Molecular Biology (Paris, France, Printed). The title of the article was 《Inhibition of phospholipase D of human platelets by protein tyrosine kinase inhibitors》.Product Details of 106392-48-7 The author mentioned the following in the article:

Protein tyrosine kinases (PTKs) of the src family are thought to play an important role in platelet signal transduction, but little is known about the targets of these enzymes in platelets. We determined that exposure of human platelets to pervanadate, an inhibitor of protein tyrosine phosphatases, caused an increase in the activity of phospholipase D (PLD), an enzyme that might be involved in signaling events leading to aggregation or secretion. To further investigate whether tyrosine phosphorylation is a step in the pathway of activation of PLD in response to thrombin, we tested the effects of a series of PTK inhibitors on the activity of platelet PLD. PLD was activated in response to 0.3 U/mL thrombin, and this activation was reduced by several of the PTK inhibitors, especially genistein, Me 2,5-dihydroxycinnamate (MDHC), ST271, and the tyrphostins A25 and A47. In saponin-permeabilized platelets, we observed a marked inhibition of GTPγS-stimulated PLD by many of the PTK inhibitors, consistent with the possibility that PTKs are involved in the regulation of PLD activity by a G-protein or small GTP-binding protein. MDHC did not affect PLD activity in permeabilized cells, which suggests that this compound might inhibit PLD in intact platelets via another pathway. The inhibitors were also tested for their effects on the phosphorylation of a peptide substrate of src-family PTKs in a platelet membrane preparation and in permeabilized platelets. Several of the compounds partially inhibited peptide phosphorylation in the membrane preparation and in permeabilized platelets, most notably ST271, ST638, and tyrphostin A25. These results suggest that the activation of PLD by thrombin during platelet stimulation is at least partially controlled by protein tyrosine kinases, possibly pp60c-src or other members of the src family. In the part of experimental materials, we found many familiar compounds, such as 2-Cyano-3-(4-hydroxy-3,5-diisopropylphenyl)acrylamide(cas: 106392-48-7Product Details of 106392-48-7)

2-Cyano-3-(4-hydroxy-3,5-diisopropylphenyl)acrylamide(cas: 106392-48-7) belongs to amides.Product Details of 106392-48-7Amides are pervasive in nature and technology. Proteins and important plastics like Nylons, Aramid, Twaron, and Kevlar are polymers whose units are connected by amide groups (polyamides); these linkages are easily formed, confer structural rigidity, and resist hydrolysis.

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

《Bioorthogonal labelling of living bacteria using unnatural amino acids containing nitrones and a nitrone derivative of vancomycin》 was written by MacKenzie, Douglas A.; Sherratt, Allison R.; Chigrinova, Mariya; Kell, Arnold J.; Pezacki, John Paul. Quality Control of tert-Butyl N,N’-diisopropylcarbamimidateThis research focused onunnatural amino acid vancomycin derivative bacterial labeling. The article conveys some information:

Unnatural D-amino acids bearing endocyclic nitrones were developed for live-cell labeling of the bacterial peptidoglycan layer. Metabolic incorporation of D-Lys and D-Ala derivatives bearing different endocyclic nitrones was observed in E. coli, L. innocua, and L. lactis. The incorporated nitrones of these bacteria then rapidly underwent strain-promoted alkyne-nitrone cycloaddition (SPANC) reactions affording chem. modified bacteria. In the experimental materials used by the author, we found tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8Quality Control of tert-Butyl N,N’-diisopropylcarbamimidate)

tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8) belongs to anime. Left-handed and right-handed forms (mirror-image configurations, known as optical isomers or enantiomers) are possible when all the substituents on the central nitrogen atom are different (i.e., the nitrogen is chiral). With amines, there is extremely rapid inversion in which the two configurations are interconverted.Quality Control of tert-Butyl N,N’-diisopropylcarbamimidate

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

Reference of (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamideOn September 30, 1985 ,《Synthesis of aldehydic peptides inhibiting renin》 was published in International Journal of Peptide & Protein Research. The article was written by Fehrentz, Jean Alain; Heitz, Annie; Castro, Bertrand. The article contains the following contents:

Peptide aldehydes R-X-X1-NHCH(CH2CHMe2)CHO (I; R = Me3CO2C (Boc), X-X1 = Phe-Phe, Val-Val, Phe-Leu; R = PhCH2O2C, X-X1 = Trp-Val, Tyr-Val, Phe-Leu) were prepared in 92-98% yields by reducing the corresponding hydroxamates R-X-X1-Leu-N(OMe)Me by LiAlH4. Peptide ketone Boc-Phe-Phe-NHCH(CH2CHMe2)COMe was prepared by treating Boc-Phe-Phe-Leu-N(OMe)Me with MeMgBr. I inhibited renin activity. The experimental process involved the reaction of (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6Reference of (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide)

(S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6) belongs to amides. Because of the greater electronegativity of oxygen, the carbonyl (C=O) is a stronger dipole than the N–C dipole. The presence of a C=O dipole and, to a lesser extent a N–C dipole, allows amides to act as H-bond acceptors.Reference of (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well.

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

《Cyanine dye mediated mitochondrial targeting enhances the anti-cancer activity of small-molecule cargoes》 was published in Chemical Communications (Cambridge, United Kingdom) in 2020. These research results belong to Nodling, Alexander R.; Mills, Emily M.; Li, Xuefei; Cardella, Davide; Sayers, Edward J.; Wu, Shih-Hsiung; Jones, Arwyn T.; Luk, Louis Y. P.; Tsai, Yu-Hsuan. Synthetic Route of C11H22N2O4 The article mentions the following:

Organelle-specific delivery systems are of significant clin. interest. The authors demonstrate the use of common cyanine dyes Cy3 and Cy5 as vectors for targeting and delivering cargoes to mitochondria in cancer cells. Specifically, conjugation to the dyes can increase cytotoxicity by up to 1000-fold. In addition to this study using H-Lys(Boc)-OH, there are many other studies that have used H-Lys(Boc)-OH(cas: 2418-95-3Synthetic Route of C11H22N2O4) was used in this study.

H-Lys(Boc)-OH(cas: 2418-95-3) belongs to amino acids. Amino acids are not generally considered to be electrochemically active because products of the oxidation accumulate on the electrode surface and prevent it from participating in any further electrochemical processes.Synthetic Route of C11H22N2O4

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

Trivella, Daniela B. B.; Pereira, Alban R.; Stein, Martin L.; Kasai, Yusuke; Byrum, Tara; Valeriote, Frederick A.; Tantillo, Dean J.; Groll, Michael; Gerwick, William H.; Moore, Bradley S. published an article in Chemistry & Biology (Oxford, United Kingdom). The title of the article was 《Enzyme inhibition by hydroamination: design and mechanism of a hybrid carmaphycin-syringolin enone proteasome inhibitor》.Recommanded Product: (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide The author mentioned the following in the article:

Hydroamination reactions involving the addition of an amine to an inactivated alkene are entropically prohibited and require strong chem. catalysts. While this synthetic process is efficient at generating substituted amines, there is no equivalent in small mol.-mediated enzyme inhibition. We report an unusual mechanism of proteasome inhibition that involves a hydroamination reaction of alkene derivatives of the epoxyketone natural product carmaphycin. We show that the carmaphycin enone first forms a hemiketal intermediate with the catalytic Thr1 residue of the proteasome before cyclization by an unanticipated intramol. alkene hydroamination reaction, resulting in a stable six-membered morpholine ring. The carmaphycin enone electrophile, which does not undergo a 1,4-Michael addition as previously observed with vinyl sulfone and α,β-unsaturated amide-based inhibitors, is partially reversible and gives insight into the design of proteasome inhibitors for cancer chemotherapy. After reading the article, we found that the author used (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6Recommanded Product: (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide)

(S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6) belongs to amides. Because of the greater electronegativity of oxygen, the carbonyl (C=O) is a stronger dipole than the N–C dipole. The presence of a C=O dipole and, to a lesser extent a N–C dipole, allows amides to act as H-bond acceptors.“,” In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well. Recommanded Product: (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide

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

Monnerat, Gustavo;Seara, Fernando A. C.;Evaristo, Joseph Albert Medeiros;Carneiro, Gabriel;Evaristo, Geisa Paulino Caprini;Domont, Gilberto;Nascimento, Jose Hamilton Matheus;Mill, Jose Geraldo;Nogueira, Fabio Cesar Souza;Campos de Carvalho, Antonio Carlos published 《Aging-related compensated hypogonadism: Role of metabolomic analysis in physiopathological and therapeutic evaluation》 in 2018. The article was appeared in 《Journal of Steroid Biochemistry and Molecular Biology》. They have made some progress in their research.Application of 2444-46-4 The article mentions the following:

Aging is a complex process that increases the risk of chronic disease development. Hormonal and metabolic alterations occur with aging, such as androgen activity decrease. Studies aim to understand the role of testosterone replacement therapy (TRT) in males, however biomarkers and the metabolic responses to TRT are not well characterized. Therefore, the present study investigated TRT effect in young adult and aged rats by metabolomics. Male Wistar rats were divided into four groups: adult and adult + testo (6 mo), old and old + testo (25-27mo). TRT animals received daily testosterone propionate (1 mg/kg/s.c.). TRT changed the testicular weight index decrease induced by aging but did not change the body weight and liver weight index. Sera were analyzed by liquid chromatograph high resolution mass spectrometry (LC-MS/MS). Testosterone was quantified by target LC-MS/MS. A total of 126 metabolites were detected with known identification altered by TRT by non-target metabolomics anal. Multivariate statistics shows that all groups segregated individually after principal component anal. The treatment with testosterone induced several metabolic alterations in adult and old rats that were summarized by variable importance on projection score, metabolite interaction and pathway anal. Aging-related hypogonadism induces a pattern of systemic metabolic alterations that can be partially reversed by TRT, however, this treatment in aged rats induces novel alterations in some metabolites that are possible new targets for monitoring in patients submitted to TRT.N-Vanillylnonanamide (cas: 2444-46-4) were involved in the experimental procedure.

N-Vanillylnonanamide(cas:2444-46-4) is a capsaicin analog that has been used to study the effects of capsaicin on energy metabolism and bowel disease.Application of 2444-46-4 It has been shown to be effective in the treatment of bowel disease, by inhibiting the production of proinflammatory cytokines and prostaglandins.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Category: amides-buliding-blocksIn 2016, Machado, Juliano;Manfredi, Leandro H.;Silveira, Wilian A.;Goncalves, Dawit A. P.;Lustrino, Danilo;Zanon, Neusa M.;Kettelhut, Isis C.;Navegantes, Luiz C. published 《Calcitonin gene-related peptide inhibits autophagic-lysosomal proteolysis through cAMP/PKA signaling in rat skeletal muscles》. 《International Journal of Biochemistry & Cell Biology》published the findings. The article contains the following contents:

Calcitonin gene-related peptide (CGRP) is a neuropeptide released by motor neuron in skeletal muscle and modulates the neuromuscular transmission by induction of synthesis and insertion of acetylcholine receptor on postsynaptic muscle membrane; however, its role in skeletal muscle protein metabolism remains unclear. We examined the in vitro and in vivo effects of CGRP on protein breakdown and signaling pathways in control skeletal muscles and muscles following denervation (DEN) in rats. In isolated muscles, CGRP (10^-10 to 10^-6 M) reduced basal and DEN-induced activation of overall proteolysis in a concentration-dependent manner. The in vitro anti-proteolytic effect of CGRP was completely abolished by CGRP8-37, a CGRP receptor antagonist. CGRP down-regulated the lysosomal proteolysis, the mRNA levels of LC3b, Gabarapl1 and cathepsin L and the protein content of LC3-II in control and denervated muscles. In parallel, CGRP elevated cAMP levels, stimulated PKA/CREB signaling and increased Foxo1 phosphorylation in both conditions. In denervated muscles and starved C2C12 cells, Rp-8-Br-cAMPs or PKI, two PKA inhibitors, completely abolished the inhibitory effect of CGRP on Foxo1, 3 and 4 and LC3 lipidation. A single injection of CGRP (100 μg kg^-1) in denervated rats increased the phosphorylation levels of CREB and Akt, inhibited Foxo transcriptional activity, the LC3 lipidation as well as the mRNA levels of LC3b and cathepsin L, two bona fide targets of Foxo. This study shows for the first time that CGRP exerts a direct inhibitory action on autophagic-lysosomal proteolysis in control and denervated skeletal muscle by recruiting cAMP/PKA signaling, effects that are related to inhibition of Foxo activity and LC3 lipidation. The experimental procedure involved many compounds, such as N-Vanillylnonanamide (cas: 2444-46-4) .

N-Vanillylnonanamide(cas:2444-46-4) has antifouling properties.Category: amides-buliding-blocks It acts as an nicotinamide adenine dinucleotide phosphate (NADPH) inhibitor.N-Vanillylnonanamide has been used for the preparation of spicules.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Goel, Reema;Reilly, Samantha M.;Valerio, Luis G. Jr. published 《A Computational Approach for Respiratory Hazard Identification of Flavor Chemicals in Tobacco Products》. The research results were published in《Chemical Research in Toxicology》 in 2022.SDS of cas: 2444-46-4 The article conveys some information:

Flavor chems. contribute to the appeal and toxicity of tobacco products, including electronic nicotine delivery systems (ENDS). The assortment of flavor chems. available for use in tobacco products is extensive. In this study, a chem.-driven computational approach was used to evaluate flavor chems. based on intrinsic hazardous structures and reactivity of chems. A large library of 3012 unique flavor chems. was compiled from publicly available information. Next, information was computed and collated based on their (1) physicochem. properties, (2) Global Harmonization System (GHS) health hazard classification, (3) structural alerts linked to the chem.’s reactivity, instability, and/or toxicity, and (4) common substructure shared with FDA’s harmful and potentially harmful constituents (HPHCs) flavor chems. that are respiratory toxicants. Computational anal. of the constructed flavor library flagged 638 chems. with GHS classified respiratory health hazards, 1079 chems. with at least one structural alert, and 2297 chems. with substructural similarity to FDA’s established and proposed list of HPHCs. A subsequent anal. was performed on a subset of 173 chems. in the flavor library that are respiratory health hazards, contain structural alerts as well as flavor HPHC substructures. Four general toxicophore structures with an increased potential for respiratory toxicity were then identified. In summary, computational methods are efficient tools for hazard identification and understanding structure-toxicity relationship. With appropriate context of use and interpretation, in silico methods may provide scientific evidence to support toxicol. evaluations of chems. in or emitted from tobacco products.N-Vanillylnonanamide (cas: 2444-46-4) were involved in the experimental procedure.

N-Vanillylnonanamide(cas:2444-46-4) has antifouling properties.SDS of cas: 2444-46-4 It acts as an nicotinamide adenine dinucleotide phosphate (NADPH) inhibitor.N-Vanillylnonanamide has been used for the preparation of spicules.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Zhang, Jing;Qian, Xing-Kai;Song, Pei-Fang;Li, Xiao-Dong;Wang, An-Qi;Huo, Hong;Yao, Jing-Chun;Zhang, Gui-Min;Zou, Li-Wei published 《A high-throughput screening assay for dipeptidyl peptidase-IV inhibitors using human plasma》 in 2021. The article was appeared in 《Analytical Methods》. They have made some progress in their research.HPLC of Formula: 2444-46-4 The article mentions the following:

Dipeptidyl peptidase-IV (DPP-IV) plays a critical role in glucose metabolism and has become an important target for type 2 diabetes mellitus. We previously reported a two-photon fluorescent probe glycyl-prolyl-N-butyl-4-amino-1,8-naphthalimide (GP-BAN) for DPP-IV detection with high specificity and sensitivity. In this study, a high-throughput screening (HTS) method for DPP-IV inhibitors using human plasma as the enzyme source was established and optimized. Further investigations demonstrate that the IC₅₀ value of sitagliptin (listed as the DPP-IV inhibitor) determined with human recombinant DPP-IV (36.22 nM) is very similar to that in human plasma (39.18 nM), and sitagliptin acts as a competitive inhibitor against human plasma DPP-IV-mediated GP-BAN hydrolysis. These results indicate that expensive human recombinant DPP-IV can be replaced by human plasma in this GP-BAN-based assay. On this basis, GP-AMC (com. probe) was used as a comparison to verify this method, and the catalytic efficacy (Vmax/Km) for GP-AMC (0.09 min^-1) hydrolysis in human plasma is lower than that for GP-BAN (0.21 min^-1). Further anal. of inhibition kinetics (sitagliptin) and mol. docking (GP-BAN and GP-AMC) showed that GP-BAN has better specificity and affinity for enzymes than GP-AMC. Finally, the optimized method was used for the HTS of DPP-IV inhibitors in 69 natural alkaloids.N-Vanillylnonanamide (cas: 2444-46-4) were involved in the experimental procedure.

N-Vanillylnonanamide(cas:2444-46-4) is a capsaicin analog that has been used to study the effects of capsaicin on energy metabolism and bowel disease.HPLC of Formula: 2444-46-4 It has been shown to be effective in the treatment of bowel disease, by inhibiting the production of proinflammatory cytokines and prostaglandins.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Heck, Rouven;Lukic, Milica Z.;Savic, Snezana D.;Daniels, Rolf;Lunter, Dominique J. published 《Ex vivo skin permeation and penetration of nonivamide from and in vivo skin tolerability of film-forming formulations containing porous silica》 in 2017. The article was appeared in 《European Journal of Pharmaceutical Sciences》. They have made some progress in their research.Category: amides-buliding-blocks The article mentions the following:

The purpose of this study was to evaluate skin permeation and penetration of nonivamide which has been formulated in novel film-forming formulations (FFFs). These formulations aim to prolong the availability of capsaicinoids which are used in long-term treatment of chronic pruritus. An oily solution of nonivamide was loaded into porous silica particles which then were suspended in an aqueous dispersion of a sustained release polymer. Permeation and penetration experiments were performed ex vivo with postauricular porcine skin using modified Franz diffusion cells. The penetrated drug amount was assessed ex vivo by skin surface biopsy followed by cryo-sectioning. Furthermore, in vivo skin irritation experiments were performed to compare the potential skin irritation caused by the FFFs to conventionally used semi-solid formulations. Permeation rates of nonivamide from FFF through the skin are comparable to that from clin. used immediate release formulations. This elucidates the therapeutic safety profile of the novel FFF. Penetration studies confirmed the prolonged drug availability at the site of action. FFFs were found not to irritate the skin of healthy volunteers. FFFs with sustained nonivamide penetration represent safe and easy-to-use formulations. They therefore may improve the treatment of chronic pruritus with capsaicinoids by enhancing patient compliance through a sustained release regime. The experimental procedure involved many compounds, such as N-Vanillylnonanamide (cas: 2444-46-4) .

N-Vanillylnonanamide(cas:2444-46-4) is a capsaicin analog that has been used to study the effects of capsaicin on energy metabolism and bowel disease.Category: amides-buliding-blocks It has been shown to be effective in the treatment of bowel disease, by inhibiting the production of proinflammatory cytokines and prostaglandins.

Reference:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics