Tag: M.W=300-400

Fliri, Anton F.; Loging, William T.; Volkmann, Robert A. published the artcile< Drug effects viewed from a signal transduction network perspective>, Product Details of C14H8N2Na2O6, the main research area is drug discovery protein network signaling.

Understanding how drugs affect cellular network structures and how resulting signals are translated into drug effects holds the key to the discovery of medicines. Herein we examine this cause-effect relationship by determining protein network structures associated with the generation of specific in vivo drug-effect patterns. Medicines having similar in vivo pharmacol. have been identified by a comparison of drug-effect profiles of 1320 medicines. Protein network positions reached by these medicines were ascertained by examining the coinvestigation frequency of these medicines and 1179 protein network constituents in millions of scientific investigations. Interestingly, medicine associations obtained by comparing by drug-effect profiles mirror those obtained by comparing drug-protein coinvestigation frequency profiles, demonstrating that these drug-protein reachability profiles are relevant to in vivo pharmacol. By using protein associations obtained in these investigations and independent, curated protein interaction information, drug-mediated protein network topol. models can be constructed. These protein network topol. models reveal that drugs having similar pharmacol. profiles reach similar discrete positions in cellular protein network systems and provide a network view of medicine cause-effect relationships.

Journal of Medicinal Chemistry published new progress about 6054-98-4. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, Product Details of C14H8N2Na2O6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Jelicic, Mario-Livio; Brusac, Edvin; Klaric, Daniela Amidzic; Nigovic, Biljana; Turk, Niksa; Mornar, Ana published the artcile< A chromatographic approach to development of 5-aminosalicylate/folic acid fixed-dose combinations for treatment of Crohn's disease and ulcerative colitis>, Quality Control of 6054-98-4, the main research area is chromatog aminosalicylate folic acid treatment Crohn disease ulcerative colitis.

Medication adherence is an important factor in inflammatory bowel disease therapy, which includes regular supplementation of malabsorbed vitamins. Absorption of folic acid is limited due to the damaging of the gastrointestinal tract, which can increase the chances to develop megaloblastic anemia and colorectal cancer. In this work, 5-aminosalicylates (mesalazine, balsalazide, sulfasalazine and olsalazine) and folic acid were characterized regarding their pharmacokinetic related properties (hydrophobicity, phospholipid and plasma protein binding) using the biomimetic chromatog. approach. Despite the high binding percentage of 5-aminosalicylates for human serum albumin (> 61.44%), results have shown that folic acid binding to human serum albumin protein is far greater (69.40%) compared to alpha 1-acid-glycoprotein (3.45%). Frontal anal. and zonal elution studies were conducted to provide an insight into the binding of folic acid to human serum albumin and potential competition with 5-aminosalicylates. The anal. method for the simultaneous determination of assay in proposed fixed-dose combinations was developed and validated according to ICH Q2 (R1) and FDA method validation guidelines. Separation of all compounds was achieved within 16 min with satisfactory resolution (Rs > 3.67) using the XBridge Ph column (150 x 4.6 mm, 3.5μm). High linearity (r > 0.9997) and precision (RSD < 2.29%) was obtained, while all recoveries were within the regulatory defined range by British (100.0 ± 5.0%) and USP (100.0 ± 10.0%). Scientific Reports published new progress about Absorption. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, Quality Control of 6054-98-4.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Cook, Ian; Leyh, Thomas S. published the artcile< The N-Terminus of Human Sulfotransferase 2B1b-a Sterol-Sensing Allosteric Site>, Recommanded Product: (3S,9S,10R,13R,14R,17R)-10,13-Dimethyl-17-((R)-6-methylheptan-2-yl)-2,3,4,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol, the main research area is sulfotransferase SULT2B1b allosteric site allostere quercetin oxysterol.

Among human cytosolic sulfotransferases, SULT2B1b is highly specific for oxysterols-oxidized cholesterol derivatives, including nuclear-receptor ligands causally linked to skin and neurodegerative diseases, cancer and atherosclerosis. Sulfonation of signaling oxysterols redirects their receptor-binding functions, and controlling these functions is expected to prove valuable in disease prevention and treatment. SULT2B1b is distinct among the human SULT2 isoforms by virtue of its atypically long N-terminus, which extends 15 residues beyond the next longest N-terminus in the family. Here, in silico studies are used to predict that the N-terminal extension forms an allosteric pocket and to identify potential allosteres. One such allostere, quercetin, is used to confirm the existence of the pocket and to demonstrate that allostere binding inhibits turnover. The structure of the pocket is obtained by positioning quercetin on the enzyme, using spin-label-triangulation NMR, followed by NMR distance-constrained mol. dynamics docking. The model is confirmed using a combination of site-directed mutagenesis and initial-rate studies. Stopped-flow ligand-binding studies demonstrate that inhibition is achieved by stabilizing the closed form of the enzyme active-site cap, which encapsulates the nucleotide, slowing its release. Finally, endogenous oxysterols are shown to bind to the site in a highly selective fashion-one of the two immediate biosynthetic precursors of cholesterol (7-dehydrocholesterol) is an inhibitor, while the other (24-dehydrocholesterol) is not. These findings provide insights into the allosteric dialogue in which SULT2B1b participates in in vivo and establishes a template against which to develop isoform-specific inhibitors to control SULT2B1b biol.

Biochemistry published new progress about Allosterism. 434-16-2 belongs to class alcohols-buliding-blocks, and the molecular formula is C27H44O, Recommanded Product: (3S,9S,10R,13R,14R,17R)-10,13-Dimethyl-17-((R)-6-methylheptan-2-yl)-2,3,4,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Speranza, Eric Demian; Colombo, Manuel; Heguilor, Santiago; Tatone, Leandro Martin; Colombo, Juan Carlos published the artcile< Alterations in the sterol signature of detritivorous fish along pollution gradients in the Rio de la Plata basin (Argentina): From plant to sewage-based diet>, Synthetic Route of 434-16-2, the main research area is sterol detritivorous fish pollution sewage diet; Coprostanol; Detritivory; Fish; Sewage; Sterols.

In order to assess the impact of sewage pollution on the diet of the strict detritivorous and migratory South American fish, Prochilodus lineatus, 16 sterol biomarkers were analyzed by gas chromatog.-mass spectrometry from fish muscle (n: 144) collected along 1200 km in the Rio de la Plata basin. Sterol concentrations were fairly homogeneous (2.4 ± 1.3 mg g-1 dry weight), but their proportion in lipids was highly variable and inversely related to both body mass and lipid contents, reflecting the more conservative character of sterols compared to the rapid accumulation of fat as fish grows. As expected, the muscle sterol signature was widely dominated by cholesterol (92 ± 4.5% of total sterols), but it exhibited a remarkable diversity with variable proportions of fecal coprostanol (4.0 ± 4.4%) and plant sterols (3.1 ± 1.9%, e.g. sitosterol and campesterol). Muscle sterols exhibited contrasting geog. differences associated with dietary shifts from plant-derived detritus in the northern reaches of the basin (N: Parana and Uruguay Rivers), to sewage dominated inputs at Buenos Aires (BA). Fish from BA are fattier (lipids: 35 ± 18 vs. 15 ± 9.0% at N), with higher total sterol contents (2.6 ± 1.3 vs. 1.9 ± 1.0 mg g-1), abundant coprostanol (5.3 ± 4.4 vs. 0.46 ± 1.1%) and lower plant sterols (2.6 ± 1.6 vs 4.6 ± 2.0%), reflecting a diet shifted to anthropogenic organic matter as opposed to vegetal detritus in the north. Accordingly, BA fish presented lower phyto/fecal sterol ratios (0.37 ± 0.21 vs. 0.91 ± 0.12 at N) and higher copro/epicoprostanol ratios (0.95 ± 0.082 vs 0.51 ± 0.25 at N), indicating fresh fecal inputs which provide a valuable supply of easily absorbed organic matter at this site. In addition, the sterol signature allowed to distinguish migratory fish from BA collected 900 km north (previously identified by their pollutant fingerprint and biochem. composition). In fact, coprostanol concentrations show a direct relationship with human populations along the basin, highlighting the usefulness of fecal sterol biomarkers as tracers of polluted fish stocks.

Environmental Research published new progress about Biomarkers. 434-16-2 belongs to class alcohols-buliding-blocks, and the molecular formula is C27H44O, Synthetic Route of 434-16-2.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Alderborn, G.; Lang, P. O.; Sagstrom, A.; Kristensen, A. published the artcile< Compression characteristics of granulated materials. I. Fragmentation propensity and compactibility of some granulations of a high dosage drug>, Safety of Sodium 5,5′-(diazene-1,2-diyl)bis(2-hydroxybenzoate), the main research area is granule compactibility fragmentation ethanol binder; azobishydroxybenzoate granule tablet property.

Three granulations of a fairly water-soluble high-dosage drug, di-Na 3,3′-azobis(6-hydroxybenzoate), were produced by intensive mixing with poly(vinylpyrrolidone), and dissolved in 3 liquids with different amounts of EtOH and water, as binder. The granulations were mixed with dry binders or with a lubricant and granulations and mixtures were compressed at 30 MPa and the tablet strength was measured. The tablet strength increased with increasing amount of EtOH in the binder solution The increase and decrease in tablet strength due to the addition of dry binder and lubricant, resp., were also dependent on the amount of EtOH in the binder solution and indicated that the degree of fragmentation varied between the granulations. Heckel plots and tablet surface area-compaction pressure profiles confirmed the finding that the degree of fragmentation of the granules increased with increasing amount of EtOH in the binding solution A good correlation between fragmentation propensity of the granulations and tensile strength of the tablets was found.

International Journal of Pharmaceutics published new progress about Pharmaceutical granules. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, Safety of Sodium 5,5′-(diazene-1,2-diyl)bis(2-hydroxybenzoate).

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Bernstein, Charles N.; Nugent, Zoann; Blanchard, James F. published the artcile< 5-Aminosalicylate Is Not Chemoprophylactic for Colorectal Cancer in IBD: A Population Based Study>, Recommanded Product: Sodium 5,5′-(diazene-1,2-diyl)bis(2-hydroxybenzoate), the main research area is Asacol chemopreventive agent prophylaxis colorectal cancer inflammatory bowel disease.

OBJECTIVES: We aimed to determine if use of 5-aminosalicylates (5-ASA) was associated with a reduced risk of colorectal cancer (CRC) in people with inflammatory bowel disease (IBD). METHODS: We used the population-based University of Manitoba IBD Epidemiol. Database that tracks all health-care visits from 1984 to 2008 of all Manitobans with IBD and all prescription medication use since 1995. In 2008, there were 8,744 subjects with IBD (ulcerative colitis 4,325, Crohn’s disease 4,419, females 4,851, males 3,893). In study I, we assessed the incidence of CRC among 5-ASA users (≥1 yr, ≥5 years of cumulative use) compared with nonusers. In study II, we assessed a cohort of those with CRC (n=101) diagnosed in 1995-2008, matched to a control cohort by age, sex, disease duration, and disease diagnosis without CRC (n=303), and logistic anal. was undertaken. RESULTS: For study I, the hazard ratio for CRC among 5-ASA users was 1.04 (95% confidence interval (CI) 0.67-1.62, P=0.87) at ≥1 yr of use and 2.01 (95% CI 1.04-3.9, P=0.038) at ≥5 years of use with no difference when assessing by diagnosis. Males, but not females, using 5-ASA for ≥5 years had an increased risk of CRC. In study II, CRC cases had similar use of any 5-ASA compared with controls for ≥1 yr of use (1.02, 95% CI 0.60-1.74) or ≥5 years (1.96, 95% CI 0.84-4.55), and a similar mean number of 5-ASA prescriptions at 10 vs. 11 (P=0.8) and a similar mean number of dose days at 330 vs. 410 (P=0.69). CONCLUSIONS: Our results support the majority of studies to date that 5-ASA is not chemoprophylactic in IBD for CRC. Am J Gastroenterol 2011; 106:731-736; doi:10.1038/ajg.2011.50; published online 15 March 2011.

American Journal of Gastroenterology published new progress about Colorectal neoplasm. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, Recommanded Product: Sodium 5,5′-(diazene-1,2-diyl)bis(2-hydroxybenzoate).

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Maines, Lynn W.; Fitzpatrick, Leo R.; French, Kevin J.; Zhuang, Yan; Xia, Zuping; Keller, Staci N.; Upson, John J.; Smith, Charles D. published the artcile< Suppression of Ulcerative Colitis in Mice by Orally Available Inhibitors of Sphingosine Kinase>, Computed Properties of 6054-98-4, the main research area is sphingosine kinase ABC294640 ABC747080 ulcerative colitis anticolitis antiinflammatory signaling.

A critical step in the mechanism of action of inflammatory cytokines is the stimulation of sphingolipid metabolism, including activation of sphingosine kinase (SK), which produces the mitogenic and proinflammatory lipid sphingosine 1-phosphate (S1P). We have developed orally bioavailable compounds that effectively inhibit SK activity in vitro in intact cells and in cancer models in vivo. In this study, we assessed the effects of these SK inhibitors on cellular responses to tumor necrosis factor alpha (TNFα) and evaluated their efficacy in the dextran sulfate sodium (DSS) model of ulcerative colitis in mice. Using several cell systems, it was shown that the SK inhibitors block the ability of TNFα to activate nuclear factor kappa B (NFκB), induce expression of adhesion proteins, and promote production of prostaglandin E2 (PGE2). In an acute model of DSS-induced ulcerative colitis, SK inhibitors were equivalent to or more effective than Dipentum in reducing disease progression, colon shortening, and neutrophil infiltration into the colon. The effects of SK inhibitors were associated with decreased colonic levels of inflammatory cytokines TNFα, interleukin (IL)-1β, interferon gamma (IFN)-γ, IL-6, and reduction of S1P levels. A similar reduction in disease progression was provided by SK inhibitors in a chronic model of ulcerative colitis in which the mice received 3-wk-long cycles of DSS interspaced with week-long recovery periods. In the chronic model, immunohistochem. for SK showed increased expression in DSS-treated mice (compared with water-treated controls) that was reduced by drug treatment. S1P levels were also elevated in the DSS group and significantly reduced by drug treatment. Together, these data indicate that SK is a critical component in inflammation and that inhibitors of this enzyme may be useful in treating inflammatory bowel diseases.

Digestive Diseases and Sciences published new progress about Anti-inflammatory agents. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, Computed Properties of 6054-98-4.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Delahunty, Ian; Li, Jianwen; Jiang, Wen; Lee, Chaebin; Yang, Xueyuan; Kumar, Anil; Liu, Zhi; Zhang, Weizhong; Xie, Jin published the artcile< 7-Dehydrocholesterol Encapsulated Polymeric Nanoparticles As a Radiation-Responsive Sensitizer for Enhancing Radiation Therapy>, COA of Formula: C27H44O, the main research area is 7-dehydrocholesterol; colon carcinoma; nanoparticles; radiation therapy; radiosensitizers.

Therapeutics that can be activated by radiation in situ to enhance the efficacy of radiotherapy are highly desirable. Herein, 7-Dehydrocholesterol (7-DHC), a biosynthetic precursor of cholesterol, as a radiosensitizer, exploiting its ability to propagate the free radical chain reaction is explored. The studies show that 7-DHC can react with radiation-induced reactive oxygen species and in turn promote lipid peroxidation, double-strand breaks, and mitochondrial damage in cancer cells. For efficient delivery, 7-DHC is encapsulated into poly(lactic-co-glycolic acid) nanoparticles, forming 7-DHC@PLGA NPs. When tested in CT26 tumor bearing mice, 7-DHC@PLGA NPs significantly enhanced the efficacy of radiotherapy, causing complete tumor eradication in 30% of the treated animals. After treatment, 7-DHC is converted to cholesterol, causing no detectable side effects or hypercalcemia. 7-DHC@PLGA NPs represent a radiation-responsive sensitizer with great potential in clin. translation.

Small published new progress about 434-16-2. 434-16-2 belongs to class alcohols-buliding-blocks, and the molecular formula is C27H44O, COA of Formula: C27H44O.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

McKay, Gordon published the artcile< Mass transport processes for the adsorption of dyes onto chitin>, HPLC of Formula: 6054-98-4, the main research area is dye adsorption chitin.

The adsorption of 4 dyestuffs onto chitin was studied. A model was developed to explain the mass transport of dyestuffs onto chitin. The 2-resistance mass transfer model is based on external film mass transfer and pore diffusion. Two solutions are presented: the first is a rapid anal. model which may be applied to adsorption systems in which the operating lines and tie lines terminate on the monolayer of the isotherm, assumed pseudo-irreversible; the second is a model which can be applied for any operating conditions but necessitates differentiation of the exptl. concentration decay curve.

Chemical Engineering and Processing published new progress about Adsorption. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, HPLC of Formula: 6054-98-4.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Carlberg, Carsten; Velleuer, Eunike published the artcile< Vitamin D and the risk for cancer: A molecular analysis>, Category: alcohols-buliding-blocks, the main research area is review colon prostate breast cancer vitamin D receptor transcriptomics; Cancer prevention; Colon cancer; Epigenome; Evolution; Immune system; Transcriptome; VDR; Vitamin D; Vitamin D response index; Vitamin D status; Vitamin D target genes.

A review. Uncontrolled overgrowth of cells, such as in cancer, is an unavoidable risk in life that affects nearly every second individual in industrialized countries. However, in part this risk can be controlled through lifestyle adjustments, such as the avoidance of smoking, unhealthy diet, obesity, phys. inactivity and other cancer risk factors. A low vitamin D status is a risk in particular for cancers of colon, prostate, breast and leukocytes. Vitamin D3 is produced non-enzymically, when the cholesterol precursor 7-dehydrocholesterol is exposed to UV-B from sunlight, i.e., all cholesterol synthesizing species, including humans, can make vitamin D3. Vitamin D endocrinol. started some 550 million years ago, when the metabolite 1α,25-dihydroxyvitamin D3 and the transcription factor vitamin D receptor teamed up for regulating the expression of hundreds of target genes in a multitude of different tissues and cell types. Initially, these genes were focused on the control of energy homeostasis, which later also involved energy-demanding innate and adaptive immunity. Rapidly growing cells of the immune system as well as those of malignant tumors rely on comparable genes and pathways, some of which are modulated by vitamin D. Accordingly, vitamin D has anti-cancer effects both directly via controlling the differentiation, proliferation and apoptosis of neoplastic cells as well as indirectly through regulating immune cells that belong to the microenvironment of malignant tumors. This review discusses effects of vitamin D on the epigenome and transcriptome of stromal and tumor cells, inter-individual variations in vitamin D responsiveness and their relation to the prevention and possible therapy of cancer.

Biochemical Pharmacology (Amsterdam, Netherlands) published new progress about Adaptive immunity. 434-16-2 belongs to class alcohols-buliding-blocks, and the molecular formula is C27H44O, Category: alcohols-buliding-blocks.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts