Category: 6054-98-4

Banda, Jagadeesh; Lakshmanan, Ramalingam; Katepalli, Ramesh Babu; Reddy Venati, Uday Kumar; Koppula, Ramesh; Shiva Prasad, V. V. S. published the artcile< Determination of mesalazine, a low bioavailability olsalazine metabolite in human plasma by UHPLC-MS/MS: Application to a pharmacokinetic study>, Name: Sodium 5,5′-(diazene-1,2-diyl)bis(2-hydroxybenzoate), the main research area is mesalazine determination blood olsalazine pharmacokinetics UHPLC mass spectrometry; Derivatization; Human plasma; LC–MS/MS; Mesalazine; Method validation; Pharmacokinetics.

Olsalazine sodium, salicylate derivative (prodrug) is effectively bioconverted to mesalazine (5-aminosalicylic acid; 5-ASA), which has an anti-inflammatory activity in ulcerative colitis. In this article, a novel highly sensitive and selective method was developed and validated to determine mesalazine in human plasma using a derivatization technique to enhance the signal intensity by using ultra-HPLC coupled to tandem mass spectrometry (UHPLC-MS/MS) with an electrospray ionization interface. The sample preparation consisted of a derivatization with propionyl anhydride followed by liquid liquid extraction (LLE) to remove the interference and minimize the matrix effect of human plasma. The multiple reaction monitoring (MRM) mode of the neg. ion was performed and the transitions of m/z 208.1→107.0 and m/z 211.1→110.1 were used to measure the derivative of mesalazine and mesalazine-d3. The chromatog. separation was achieved using kinetex XB-C18 (100 × 4.6 mm 2.6 μ) anal. column with 0.1% formic acid in water and acetonitrile as mobile phase with a gradient elution. Nominal retention times of mesalazine and IS were 3.08 and 3.07 min, resp. Absolute recovery was found to be between 82-95% for analyte and about 78% for IS. The standard curves was linear (R2 > 0.995) in the concentration range 0.10 to 12.0 ng/mL with lower limit of quantification (LLOQ) in human plasma was 0.10 ng/mL. The average intra-day/inter-day precision values (%CV) were in the range from 0.6-2.9 % and 1.3-3.8 %, resp., while the average accuracy value was 103.8-107.2%. This method has been successfully applied to the human pharmacokinetics of olsalazine sodium 250 mg capsules following single oral administration.

Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences published new progress about Anti-inflammatory agents. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, Name: Sodium 5,5′-(diazene-1,2-diyl)bis(2-hydroxybenzoate).

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Maines, Lynn W.; Fitzpatrick, Leo R.; Green, Cecelia L.; Zhuang, Yan; Smith, Charles D. published the artcile< Efficacy of a novel sphingosine kinase inhibitor in experimental Crohn's disease>, COA of Formula: C14H8N2Na2O6, the main research area is sphingosine kinase inhibitor ABC294640 colon edema cytokine Crohns disease.

Aim: Activation of sphingosine kinase (SK) is a key response to many inflammatory processes. The present studies test the hypothesis that an orally available SK inhibitor, ABC294640, would be effective in rodent models of Crohn’s disease. Methods: Trinitrobenzene sulfonic acid (TNBS) was administered rectally to mice and rats. Rats were treated with ABC294640 orally alone or in combination with olsalazine and disease progression was monitored. Results: For both rodent species, treatment with ABC294640 attenuated disease progression. Colon samples from the ABC294640-treated animals had improved histol. and cytokine parameters when compared with vehicle-treated animals. The expression of SK was similarly increased in TNBS-treated animals and in human colon tissue specimens from inflammatory bowel disease patients relative to normal, control patients. Conclusions: Sphingosine kinase may be a critical mediator of colonic damage during intestinal inflammation, and pharmacol. inhibitors of this enzyme may prove useful in the treatment of Crohn’s disease.

Inflammopharmacology published new progress about Body weight. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, COA of Formula: C14H8N2Na2O6.

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Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Jeong, Eun-mi; Lee, Mi Young; Lee, Jeong Hyun; Lee, Byung Ho; Oh, Kwang-Seok published the artcile< A dual readout assay based on fluorescence polarization and time-resolved fluorescence resonance energy transfer to screen for RSK1 inhibitors>, Computed Properties of 6054-98-4, the main research area is ribosomal S6 kinase 1 inhibitor dual readout assay.

A dual readout assay based on fluorescence polarization (FP) and time-resolved fluorescence resonance energy transfer (TR-FRET) exhibits many advantages over single assay technol. in terms of screening quality and efficiency. In this study, we developed a dual readout assay combining FP and TR-FRET to identify ribosomal S6 kinase 1 (RSK1) inhibitors. This dual readout assay can monitor both FP and TR-FRET signals from a single RSK1 kinase reaction by using the immobilized metal affinity for phosphochem. (IMAP)-based assay. The Z’ value and signal to background (S/B) ratio were 0.85 and 4.0 using FP, and 0.79 and 10.6 using TR-FRET, which led to performance of a pilot library screening against the drug repositioning set consisting of 2320 compounds with a reasonable reproducibility. From this screening, we identified 16 compounds showing greater than 50% inhibition against RSK1 for both FP and TR-FRET; 6 compounds with greater than 50% inhibition only for FP; and 4 compounds with greater than 50% inhibition only for TR-FRET. In a cell-based functional assay to validate the hit compounds, 10 compounds identified only in a single assay had little effect on the RSK-mediated phosphorylation of liver kinase B1, whereas 5 compounds showing greater than 80% inhibition for both FP and TR-FRET reduced the phosphorylation of liver kinase B1. These results demonstrate that the dual readout assay can be used to identify hit compounds by subsequently monitoring both FP and TR-FRET signals from one RSK1 reaction.

Biological & Pharmaceutical Bulletin published new progress about Homo sapiens. 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

Heng, Ya Gao; Wen, Li Peng; Pan, Pan Meng; Xue, Feng Feng; Jian, Qiang Li; Hui, Qiong Wu; Chang, Sheng Yan; Yang, Yang Xiong; Luo, Feng published the artcile< Lanthanide separation using size-selective crystallization of Ln-MOFs>, Formula: C14H8N2Na2O6, the main research area is size selective crystallization separation lanthanide olsalazine MOF; crystal structure lanthanide olsalazine MOF preparation.

Herein, the authors report an elaborate method, size-selective crystallization of Ln-MOFs, to isolate lanthanide (Ln) ions. Herein, 13 lanthanide ions, except for the radioactive Pm(III) ion and ytterbium, were separated by four types of Ln-MOFs: type I [La-Pr, Ln2(OLZ)(H2OLZ)(DMF)(H2O)2·2H2O], type II [Nd-Eu, Ln(OLZ)0.5(H2OLZ)0.5(DMF)(μ2-DMF)0.5], type III [Gd-Ho, Ln(OLZ)0.5(H2OLZ)0.5(DMF)(H2O)·H2O], and type IV [Er-Lu, Ln2(OLZ)(H2OLZ)(H2O)4 where OLZ = olsalazine]. Further systemic investigation also suggested the highly selective separation of lanthanide ions by this method.

Chemical Communications (Cambridge, United Kingdom) published new progress about Crystal structure. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, Formula: C14H8N2Na2O6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Levinson, Robert A. published the artcile< Disodium azodisalicylate>, Safety of Sodium 5,5′-(diazene-1,2-diyl)bis(2-hydroxybenzoate), the main research area is review azodisalicylate inflammatory bowel disease.

A review with 22 references on the use of azodisalicylate (I) [6054-98-4] in the treatment of inflammatory bowel disease.

American Journal of Gastroenterology published new progress about Inflammatory bowel disease. 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

Rubin, David T.; LoSavio, Andelka; Yadron, Nicole; Huo, Dezheng; Hanauer, Stephen B. published the artcile< Aminosalicylate therapy in the prevention of dysplasia and colorectal cancer in ulcerative colitis>, Application In Synthesis of 6054-98-4, the main research area is dysplasia colorectal cancer ulcerative colitis asacol dipentum azulfidine antitumor.

Background & Aims: Aminosalicylates have been suggested as chemopreventive agents for colorectal cancer (CRC) in ulcerative colitis (UC). We studied the effect of aminosalicylate use on dysplasia and CRC risk in chronic UC. Methods: UC patients with dysplasia or CRC were matched with controls by disease duration, extent, and age at diagnosis. The total amount of aminosalicylates over the duration of the disease and the mean daily amount of drug was calculated Conditional logistic regression was used to examine the relationship of aminosalicylates to the risk of neoplasia; potential confounders were controlled in a multivariable model. Results: Twenty-six cases (8 CRC, 18 dysplasia) were matched with 96 controls. Cases and controls were similar in age (median, 43 vs 42.5 y), age at diagnosis of UC (median, 29.5 vs 30.5 y), duration of UC (median, 11.5 vs 9 y), and extent of disease (58% pancolitis), sex, family history of UC, history of primary sclerosing cholangitis, and smoking history. Cases were more likely to have a family history of CRC than controls (27% of cases, 9% of controls, P = .036). Conditional logistic regression adjusted for disease duration, age at diagnosis, and family history of CRC showed that aminosalicylate use of 1.2 g/day or more was associated with a 72% reduction in the odds of dysplasia/CRC (odds ratio, 0.28; 95% confidence interval, 0.09-0.85). As the total dose of aminosalicylates increased, the odds of dysplasia/CRC decreased (P = .056). Conclusions: This case-control study shows a significant risk reduction of dysplasia and CRC in UC patients exposed to aminosalicylate therapy.

Clinical Gastroenterology and Hepatology published new progress about Antitumor agents. 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, Application In Synthesis of 6054-98-4.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Wikberg, Martin; Alderborn, Goeran published the artcile< Compression characteristics of granulated materials. IV. The effect of granule porosity on the fragmentation propensity and the compactibility of some granulations>, Application of C14H8N2Na2O6, the main research area is granulation granule porosity fragmentation compactibility; compression granulation tablet property.

Eleven granulations of a common filler (lactose) and 3 granulations of a high-dosage drug (dipentum) were produced by wet granulation with poly(vinylpyrrolidone) as binder in a high shear mixer. The agglomeration process was varied to produce granulations with varying granule porosity. The size fraction 500-710 μm was separated and characterized on binder content (lactose granulations), granule porosity and friability. The granule fragmentation during compaction was evaluated by measurements of the air permeability of the tablets. Finally, the diametral compression strength of tablets compacted from unlubricated granulations and lactose granulations lubricated with 0.5% by weight magnesium stearate at 150 MPa was measured. The results showed that the degree of granule fragmentation during compaction was related to the granule porosity before compaction. A granulation with a higher porosity had a higher fragmentation propensity, as evaluated by the permeametry measurements, and the tablet strength was less affected by magnesium stearate addition The tablet strength correlated well with the degree of fragmentation, i.e. a granulation with higher degree of fragmentation gave tablets of a higher mech. strength. Variations in compactibility, when the same formulation is wet granulated under different process conditions, can be explained by variations in granule porosity.

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, Application of C14H8N2Na2O6.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Mahmud, N.; O’Toole, D.; O’Hare, N.; Freyne, P. J.; Weir, D. G.; Kelleher, D. published the artcile< Evaluation of renal function following treatment with 5-aminosalicylic acid derivatives in patients with ulcerative colitis>, SDS of cas: 6054-98-4, the main research area is mesalazine olsalazine aminosalicylate ulcerative colitis nephrotoxicity microalbuminuria prognosis.

A number of cases of nephrotoxicity have been reported in patients with inflammatory bowel disease taking oral 5-aminosalicylic acid (5-ASA). The aim of this study was to evaluate the effects of 9 mo of therapy with mesalazine or olsalazine on renal function in patients with ulcerative colitis in remission. Forty patients with ulcerative colitis in complete remission for 6 mo were randomized to either olsalazine (n = 20) or mesalazine (n = 20 for nine months). Thirty-six of the 40 patients were on prior salicylate therapy. Disease activity was the measure of clin. efficacy and was assessed by the Harvey-Bradshaw Index (HBI). Laboratory efficacy measurements included glomerular filtration rate (GFR), microalbuminuria, urinary glutathione S-transferase (GST) and serum C-reactive protein (CRP). Safety anal. consisted of documentation of adverse events and laboratory values. There was no significant reduction in the GFR overall on therapy. The levels of GFR adjusted for baseline were similar in the two treatment groups after 3, 6 and 9 mo. A significantly higher percentage of mesalazine-treated patients experienced drug related adverse events, all of a minor nature. The incidence of adverse events causing early withdrawal was similar in the two treatment groups. Treatment with mesalazine or olsalazine for 9 mo had no significant impact on GFR.

Alimentary Pharmacology and Therapeutics published new progress about C-reactive protein Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, SDS of cas: 6054-98-4.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Mahmud, N.; O’Toole, D.; O’Hare, N.; Freyne, P. J.; Weir, D. G.; Kelleher, D. published the artcile< Evaluation of renal function following treatment with 5-aminosalicylic acid derivatives in patients with ulcerative colitis>, SDS of cas: 6054-98-4, the main research area is mesalazine olsalazine aminosalicylate ulcerative colitis nephrotoxicity microalbuminuria prognosis.

A number of cases of nephrotoxicity have been reported in patients with inflammatory bowel disease taking oral 5-aminosalicylic acid (5-ASA). The aim of this study was to evaluate the effects of 9 mo of therapy with mesalazine or olsalazine on renal function in patients with ulcerative colitis in remission. Forty patients with ulcerative colitis in complete remission for 6 mo were randomized to either olsalazine (n = 20) or mesalazine (n = 20 for nine months). Thirty-six of the 40 patients were on prior salicylate therapy. Disease activity was the measure of clin. efficacy and was assessed by the Harvey-Bradshaw Index (HBI). Laboratory efficacy measurements included glomerular filtration rate (GFR), microalbuminuria, urinary glutathione S-transferase (GST) and serum C-reactive protein (CRP). Safety anal. consisted of documentation of adverse events and laboratory values. There was no significant reduction in the GFR overall on therapy. The levels of GFR adjusted for baseline were similar in the two treatment groups after 3, 6 and 9 mo. A significantly higher percentage of mesalazine-treated patients experienced drug related adverse events, all of a minor nature. The incidence of adverse events causing early withdrawal was similar in the two treatment groups. Treatment with mesalazine or olsalazine for 9 mo had no significant impact on GFR.

Alimentary Pharmacology and Therapeutics published new progress about C-reactive protein Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 6054-98-4 belongs to class alcohols-buliding-blocks, and the molecular formula is C14H8N2Na2O6, SDS of cas: 6054-98-4.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

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