Tag: M.W=200-250

Jowett, Laura A.; Howe, Ethan N. W.; Soto-Cerrato, Vanessa; Van Rossom, Wim; Perez-Tomas, Ricardo; Gale, Philip A. published the artcile< Indole-based perenosins as highly potent HCl transporters and potential anti-cancer agents>, Quality Control of 35564-86-4, the main research area is breast cancer perenosin hydrogen chloride transporter anticancer cytotoxicity.

Prodigiosin is one of the most potent anion transporters in lipid bilayer membranes reported to date. Inspired by the structure of this natural product, we have recently designed and synthesized a new class of H+/Cl- cotransporters named ‘perenosins’. Here we report a new library of indole-based perenosins and their anion transport properties. The new transporters demonstrated superior transmembrane transport efficiency when compared to other indole-based transporters, due to favorable encapsulating effects from the substituents on the perenosin backbone. Anion transport assays were used to determine the mechanism of chloride transport revealing that the compounds function as ‘strict’ HCl cotransporters. Cell viability studies showed that some compounds specifically trigger late-onset cell death after 72 h with a unique correlation to the position of alkyl chains on the perenosins. Further investigations of cell death mechanism showed a mixture of cell cycle arrest and apoptosis was responsible for the observed decrease in cell viability.

Scientific Reports published new progress about Antitumor agents. 35564-86-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C7H18ClNO5, Quality Control of 35564-86-4.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Zhang, Zheng; Yu, Haijie; Huang, Junhao; Faouzi, Malika; Schmitz, Carsten; Penner, Reinhold; Fleig, Andrea published the artcile< The TRPM6 Kinase Domain Determines the Mg·ATP Sensitivity of TRPM7/M6 Heteromeric Ion Channels>, Recommanded Product: N-Methyl-D-glucamine Hydrochloride, the main research area is TRPM6 kinase magnesium ATP TRPM7 heteromer ion channel human; Magnesium; Metabolic Regulation; Protein Complexes; Protein Kinases; TRP channels.

The transient receptor potential melastatin member 7 (TRPM7) and member 6 (TRPM6) are divalent cation channel kinases essential for magnesium (Mg2+) homeostasis in vertebrates. It remains unclear how TRPM6 affects divalent cation transport and whether this involves functional homomeric TRPM6 plasma membrane channels or heteromeric channel assemblies with TRPM7. We show that homomeric TRPM6 is highly sensitive to intracellular free Mg2+ and therefore unlikely to be active at physiol. levels of [Mg2+]i. Co-expression of TRPM7 and TRPM6 produces heteromeric TRPM7/M6 channels with altered pharmacol. and sensitivity to intracellular Mg·ATP compared with homomeric TRPM7. Strikingly, the activity of heteromeric TRPM7/M6 channels is independent of intracellular Mg·ATP concentrations, essentially uncoupling channel activity from cellular energy status. Disruption of TRPM6 kinase phosphorylation activity re-introduces Mg·ATP sensitivity to the heteromeric channel similar to that of TRPM7. Thus, TRPM6 modulates the functionality of TRPM7, and the TRPM6 kinase plays a critical role in tuning the phenotype of the TRPM7·M6 channel complex.

Journal of Biological Chemistry published new progress about Biological cation transport. 35564-86-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C7H18ClNO5, Recommanded Product: N-Methyl-D-glucamine Hydrochloride.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Brindle, Joseph S.; Nelson, Patrick S.; Charde, Rashmi P.; Sufyan, Sayed Abu; Nigra, Michael M. published the artcile< Catalytic cooperativity between glucose oxidase and gold nanoparticles in the sequential oxidation of glucose to saccharic acid>, SDS of cas: 87-73-0, the main research area is nanoparticle enzyme catalytic biomass glucose saccharic acid transition state; glucose gold nanoparticle catalyst oxidation saccharic acid oxidase.

There exists great potential in combining heterogeneous metallic nanoparticle active sites and enzymic active sites for sequentially catalyzed chem. transformations. This study provides an illustrative system where glucose oxidase and gold nanoparticles are successfully combined into a hybrid catalytic material. This multi-site catalyst is used to convert glucose to a more valuable saccharic acid product without the need for a strong oxidant such as H2O2, hypochlorite, or nitric acid to be externally added. We synthesize a hybrid material that is able to oxidize glucose to gluconic acid and H2O2 with glucose oxidase, and gold catalyzes the further oxidation to saccharic acid. The in situ generation of H2O2 provides a proximal, dilute oxidizing agent for further oxidation It is observed that higher pH promotes H2O2 decomposition and saccharic acid generation catalyzed by the gold nanoparticles. A 33% yield of saccharic acid in 90 min is observed without the addition of nitric acid, harsh oxidant, above ambient temperatures, or high oxygen pressures. The results demonstrate a cooperative reaction cascade system that opens new possibilities for metal nanoparticle-enzyme hybrid materials that can be applied to catalytic biomass conversion in mild reaction conditions.

Green Chemistry published new progress about Nanoparticles. 87-73-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C6H10O8, SDS of cas: 87-73-0.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Labarthe, Benoit; Idee, Jean-Marc; Burnett, Roger; Corot, Claire published the artcile< In Vivo Comparative Antithrombotic Effects of Ioxaglate and Iohexol and Interaction With the Platelet Antiaggregant Clopidogrel>, Synthetic Route of 35564-86-4, the main research area is ionic nonionic contrast media antithrombotic interaction clopidogrel.

RATIONALE AND OBJECTIVES. Experiments were designed to (1) compare the effects of iodinated contrast media (CM) on a rat model of arterial thrombosis, (2) evaluate which element of the ioxaglate solution supports its antithrombotic activity, and (3) investigate the interaction of ionic and non-ionic CM with the antiplatelet agent clopidogrel. MATERIALS AND METHODS. Carotid thrombosis was induced in rats by extravascular application of a filter paper soaked in FeCl (35% vol/wt), proximal to an ultrasonic flow probe. (1) The antithrombotic potential of low-osmolar ionic (ioxaglate Na/meglumine) or nonionic contrast media (iohexol and iodixanol) (all 1600 mg iodine/kg, IV) was assessed by measuring the time to occlusion (TTO) of the carotid artery and the thrombus weight (TW). (2) Isotonic saline and iso-osmolar (280 mOsm/kg) and hyperosmolar (560 mOsm/kg) solutions of meglumine hydrochloride, meglumine ioxaglate (560 mOsm/kg), sodium ioxaglate (600 mOsm/kg) and sodium and meglumine ioxaglate (com. solution) were tested under similar conditions. (3) Interaction with clopidogrel was tested by injecting lower dose of CM (960 mg iodine/kg) 2 h after clopidogrel (2 mg/kg per os). RESULTS: (1) Ioxaglate prolonged TTO when compared with saline (30.0 ± 1.1 min vs. 19.6 ± 2.4 min, <0.001), whereas iohexol had no effect (21.3 ± 1.3 min). Ioxaglate's effect was associated with a reduction in TW with ioxaglate vs. saline (2.6 ± 0.4 mg and 4.7 ± 0.7 mg, resp., <0.05) whereas TW remained unchanged in the iohexol group (4.2 ± 0.4 mg). The nonionic dimer iodixanol induced a direct vasoconstrictor effect on the carotid artery and was consequently excluded from the study. (2) Neither iso-osmolar nor hyperosmolar solutions of meglumine had any effect on TTO whereas both sodium and meglumine salts of ioxaglic acid prolonged TTO, suggesting that the antithrombotic effect of ioxaglate is mediated by the ioxaglic acid moiety alone as neither meglumine, osmolality or sodium played a significant role. (3) A synergistic effect on TTO was found when ioxaglate was associated with clopidogrel whereas no such effect was observed with iohexol. CONCLUSIONS: These data show a greater in vivo antithrombotic potential for the ionic contrast medium ioxaglate than for the non-ionic contrast medium iohexol and, for the first time, a synergistic effect between a contrast medium and a platelet antiaggregant drug in vivo. Investigative Radiology published new progress about Anticoagulants. 35564-86-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C7H18ClNO5, Synthetic Route of 35564-86-4.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Hou, Jianshen; Gao, Cong; Guo, Liang; Nielsen, Jens; Ding, Qiang; Tang, Wenxiu; Hu, Guipeng; Chen, Xiulai; Liu, Liming published the artcile< Rewiring carbon flux in Escherichia coli using a bifunctional molecular switch>, Category: alcohols-buliding-blocks, the main research area is glucaric acid shikimic acid Escherichia coli metabolic engineering; Dynamic regulation; Metabolic engineering; Metabolic flux regulation; Synthetic biology.

The unbalanced distribution of carbon flux in microbial cell factories can lead to inefficient production and poor cell growth. Uncoupling cell growth and chem. synthesis can therefore improve microbial cell factory efficiency. Such uncoupling, which requires precise manipulation of carbon fluxes, can be achieved by up-regulating or down-regulating the expression of enzymes of various pathways. In this study, a dynamic turn-off switch (dTFS) and a dynamic turn-on switch (dTNS) were constructed using growth phase-dependent promoters and degrons. By combining the dTFS and dTNS, a bifunctional mol. switch that could orthogonally regulate two target proteins was introduced. This bifunctional mol. switch was used to uncouple cell growth from shikimic acid and D-glucaric acid synthesis, resulting in the production of 14.33 g/L shikimic acid and the highest reported productivity of D-glucaric acid (0.0325 g/L/h) in Escherichia coli MG1655. This proved that the bifunctional mol. switch could rewire carbon fluxes by controlling target protein abundance.

Metabolic Engineering published new progress about Escherichia coli. 87-73-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C6H10O8, Category: alcohols-buliding-blocks.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Rahman, Habibur Md.; Akter, Rokeya; Bhattacharya, Tanima; Abdel-Daim, Mohamed M.; Alkahtani, Saad; Arafah, Mohammed W.; Al-Johani, Norah S.; Alhoshani, Norah M.; Alkeraishan, Nora; Alhenaky, Alhanof; Abd-Elkader, Omar H.; El-Seedi, Hesham R.; Kaushik, Deepak; Mittal, Vineet published the artcile< Resveratrol and neuroprotection: impact and its therapeutic potential in Alzheimer's disease>, Reference of 501-36-0 , the main research area is review resveratrol neuroprotection Alzheimer disease; Alzheimer’s disease; bioavailability; neuroprotective; oxidative stress; resveratrol; therapeutic agent.

A review. Alzheimer’s disease (AD) is a progressive cortex and hippocampal neurodegenerative disease which ultimately causes cognitively impaired decline in patients. The AD pathogen is a very complex process, including aggregation of Aβ (β-amyloid peptides), phosphorylation of tau-proteins, and chronic inflammation. Exactly, resveratrol, a polyphenol present in red wine, and many plants are indicated to show the neuroprotective effect on mechanisms mostly above. Resveratrol plays an important role in promotion of non-amyloidogenic cleavage of the amyloid precursor protein. It also enhances the clearance of amyloid beta-peptides and reduces the damage of neurons. Most exptl. research on AD and resveratrol has been performed in many species, both in vitro and in vivo, during the last few years. Nevertheless, resveratrol’s effects are restricted by its bioavailability in the reservoir. Therefore, scientists have tried to improve its efficiency by using different methods. This review focuses on recent work done on the cell and animal cultures and also focuses on the neuroprotective mol. mechanisms of resveratrol. It also discusses about the therapeutic potential onto the treatment of AD.

Frontiers in Pharmacology published new progress about Alzheimer disease. 501-36-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H12O3, Reference of 501-36-0 .

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Chen, Jian Jeffrey; Liu, Qingyian; Yuan, Chester; Gore, Vijay; Lopez, Patricia; Ma, Vu; Amegadzie, Albert; Qian, Wenyuan; Judd, Ted C.; Minatti, Ana E.; Brown, James; Cheng, Yuan; Xue, May; Zhong, Wenge; Dineen, Thomas A.; Epstein, Oleg; Human, Jason; Kreiman, Charles; Marx, Isaac; Weiss, Matthew M.; Hitchcock, Stephen A.; Powers, Timothy S.; Chen, Kui; Wen, Paul H.; Whittington, Douglas A.; Cheng, Alan C.; Bartberger, Michael D.; Hickman, Dean; Werner, Jonathan A.; Vargas, Hugo M.; Everds, Nancy E.; Vonderfecht, Steven L.; Dunn, Robert T. II; Wood, Stephen; Fremeau, Robert T. Jr.; White, Ryan D.; Patel, Vinod F. published the artcile< Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer's disease>, Computed Properties of 660867-80-1, the main research area is aminooxazoline azaxanthene derivative preparation oral beta secretase inhibitor Alzheimer’s; 3-Azaxanthene; Alzheimer’s disease (AD); Aminooxazoline; Amyloid; Aβ peptides; Xanthene; β-Secretase (BACE1).

The β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer’s disease. We used a structure- and property-based drug design approach to identify 2-aminooxazoline 3-azaxanthenes as potent BACE1 inhibitors which significantly reduced CSF and brain Aβ levels in a rat pharmacodynamic model. Compared to the initial lead 2, compound 28 exhibited reduced potential for QTc prolongation in a non-human primate cardiovascular safety model.

Bioorganic & Medicinal Chemistry Letters published new progress about Alzheimer disease. 660867-80-1 belongs to class alcohols-buliding-blocks, and the molecular formula is C12H18BNO2, Computed Properties of 660867-80-1.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Tian, Ya-Ming; Guo, Xiao-Ning; Krummenacher, Ivo; Wu, Zhu; Nitsch, Joern; Braunschweig, Holger; Radius, Udo; Marder, Todd B. published the artcile< Visible-Light-Induced Ni-Catalyzed Radical Borylation of Chloroarenes>, Safety of 2-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine, the main research area is chloro nickel carbene preparation catalyzed radical borylation chloroarene; crystal structure imidazolylidene nickel chloride; mol structure imidazolylidene nickel chloride; arylborane preparation.

A highly selective and general photoinduced C-Cl borylation protocol that employs [Ni(IMes)2] (IMes = 1,3-dimesitylimidazoline-2-ylidene) for the radical borylation of chloroarenes is reported. This photoinduced system operates with visible light (400 nm) and achieves borylation of a wide range of chloroarenes with B2pin2 at room temperature in excellent yields and with high selectivity, thereby demonstrating its broad utility and functional group tolerance. Mechanistic studies suggest that the borylation reactions proceed via a radical process. EPR studies demonstrate that [Ni(IMes)2] undergoes very fast Cl atom abstraction from aryl chlorides to give [Ni(I)(IMes)2Cl] and aryl radicals. Control experiments indicate that light promotes the reaction of [Ni(I)(IMes)2Cl] with aryl chlorides generating addnl. aryl radicals and [Ni(II)(IMes)2Cl2]. The aryl radicals react with an anionic sp2-sp3 diborane [B2pin2(OMe)]- formed from B2pin2 and KOMe to yield the corresponding borylation product and the [Bpin(OMe)]•- radical anion, which reduces [Ni(II)(IMes)2Cl2] under irradiation to regenerate [Ni(I)(IMes)2Cl] and [Ni(IMes)2] for the next catalytic cycle.

Journal of the American Chemical Society published new progress about Aryl chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 660867-80-1 belongs to class alcohols-buliding-blocks, and the molecular formula is C12H18BNO2, Safety of 2-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Dong, Yan; Li, Kehuang; Xu, Zhixiang; Ma, Haikuo; Zheng, Jiyue; Hu, Zhilin; He, Sudan; Wu, Yiyuan; Sun, Zhijian; Luo, Lusong; Li, Jiajun; Zhang, Hongjian; Zhang, Xiaohu published the artcile< Exploration of the linkage elements of porcupine antagonists led to potent Wnt signaling pathway inhibitors>, Product Details of C12H18BNO2, the main research area is protein palmitoyltransferase Porcupine antagonist synthesis inhibitor Wnt signaling secretion; Antagonist; Cancer therapy; Porcupine; Scaffold hybridization; Wnt signaling pathway.

The Wnt signaling pathway is a pivotal developmental pathway. It operates through control of cellular functions such as proliferation, differentiation, migration and polarity. Aberrant Wnt signaling has been implicated in the formation and metastasis of tumors. Porcupine is a component of the Wnt signaling pathway. It is a member of the membrane-bound O-acyltransferase family of proteins. Porcupine catalyzes the palmitoylation of Wnt proteins, a process which is essential to their secretion and activity. Here we report a novel series of compounds obtained by a scaffold hybridization strategy from two known porcupine inhibitor classes. The leading compound 62 demonstrated subnanomolar (IC50 0.11 nM) inhibition of Wnt signaling in a paracrine cellular reporter gene assay. Compound 62 also potently inhibited Wnt secretion into culture medium, an indication of direct inhibition of the porcupine protein. Furthermore, compound 62 showed excellent chem., plasma and liver microsomal stabilities. Collectively, these results strongly support further optimization of this novel scaffold to develop better Wnt pathway inhibitors.

Bioorganic & Medicinal Chemistry published new progress about Amide group (in Porcupine antagonists). 660867-80-1 belongs to class alcohols-buliding-blocks, and the molecular formula is C12H18BNO2, Product Details of C12H18BNO2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Tohya, Mari; Watanabe, Shin; Teramoto, Kanae; Uechi, Kohei; Tada, Tatsuya; Kuwahara-Arai, Kyoko; Kinjo, Takeshi; Maeda, Shiro; Nakasone, Isamu; Zaw, Ni Ni; Mya, San; Zan, Khin Nyein; Tin, Htay Htay; Fujita, Jiro; Kirikae, Teruo published the artcile< Pseudomonas asiatica sp. nov., isolated from hospitalized patients in Japan and Myanmar>, Product Details of C6H10O8, the main research area is Pseudomonas 16S rRNA phylogeny; Pseudomonas; human pathogen.

A novel Gram-neg., aerobic, rod-shaped, non-spore-forming bacterial strain, RYU5T, was isolated from a stool sample of an inpatient at a hospital in Okinawa, Japan. The optimal growth temperature of RYU5T was 30°C. Phylogenetic anal. based on the sequences of housekeeping genes, including the 16S rRNA, rpoB, rpoD and gyrB genes, showed that RYU5T was a member of the Pseudomonas putida group and was located close to Pseudomonas monteilii and P. putida. Whole-genome comparisons, using average nucleotide identity and digital DNA-DNA hybridization, confirmed that strain RYU5T should be classified as a novel species of Pseudomonas. Phenotypic characterization tests showed that utilization of d-mannose, d-serine, l-arabinose and d-fructose could distinguish this strain from other related species of the genus Pseudomonas. Based on genetic and phenotypic evidence, strain RYU5T should be classified as a novel species, for which the name Pseudomonas asiatica sp. nov. is proposed. The type strain is RYU5T (= DSM 107182T, = JCM 32716T), with a DNA G + C content of 62.25 mol%.

International Journal of Systematic and Evolutionary Microbiology published new progress about 16S rRNA Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 87-73-0 belongs to class alcohols-buliding-blocks, and the molecular formula is C6H10O8, Product Details of C6H10O8.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts