Category: 117976-90-6

High-Throughput Screening Assays for Cancer Immunotherapy Targets: Ectonucleotidases CD39 and CD73 was written by Kumar, Meera;Lowery, Robert;Kumar, Vaishnav. And the article was included in SLAS Discovery in 2020.Category: imidazoles-derivatives The following contents are mentioned in the article:

Production of adenosine in the extracellular tumor microenvironment elicits strong immunosuppression and is associated with tumor progression. Thus, targeting adenosine-generating ectonucleotidases is a potential strategy to stimulate and prolong antitumor immunity. Because the reaction products of ectonucleotidases differ by a single phosphate group, selective detection in an assay format that is compatible with high-throughput screening (HTS) has been elusive. We report the development of biochem. assays capable of measuring the activity of ectonucleoside triphosphate diphosphohydrolase-1 (ENTPD1; also known as CD39) and ecto-5′-nucleotidase (CD73). Both assays leverage the Transcreener HTS Assay platform, which facilitates selective immunodetection of nucleotides with homogenous fluorescent readouts, fluorescence polarization or time-resolved fluorescence energy transfer. The Transcreener AMP2 Assay was used to measure CD39 activity, allowing detection of adenosine monophosphate (AMP) production (Z> 0.6) with subnanomolar amounts of CD39, allowing IC50 determination for tool compounds, consistent with previously reported values. To detect the production of adenosine by CD73, the Transcreener ADP2 Assay was coupled with adenosine kinase (AK); conversion of adenosine to AMP and ADP (ADP) by AK allows detection with ADP2 antibody. The Transcreener AMP2 Assay was used to screen a 1280 Library of Pharmacol. Active Compounds (LOPAC) library and a 1600-compound subset of a ChemBridge diversity library for CD39 inhibitors, allowing the identification of nine and eight candidate compounds from each library, resp. The Transcreener ADP2 Assay was used to screen 1600 compounds from the ChemBridge diversity library for CD73 inhibitors and identified 14 potential candidates. HTS-compatible assays for ectonucleotidase activity may allow identification of purinergic signaling pathway inhibitors important for tumor-specific immune responses during tumor pathogenesis. This study involved multiple reactions and reactants, such as Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6Category: imidazoles-derivatives).

Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6) belongs to imidazole derivatives. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole has become an important synthon in the development of new drugs. Imidazole based anticancer drug find applications in cancer chemotherapy. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC).Category: imidazoles-derivatives

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Rabeprazole plus amoxicillin dual therapy is equally effective to bismuth-containing quadruple therapy for Helicobacter pylori eradication in central China: A single-center, prospective, open-label, randomized-controlled trial was written by Shao, Qiao-Qiao;Yu, Xue-Chun;Yu, Miao;Ma, Jing;Zhao, Jun-Bo;Yuan, Lin;Qi, Ya-Bin;Hu, Ruo-Bing;Wei, Pei-Ru;Xiao, Wei;Lan, Ling;Jia, Bai-Ling;Zhang, Lian-Zhong;Ding, Song-Ze. And the article was included in Helicobacter in 2022.Formula: C18H20N3NaO3S The following contents are mentioned in the article:

Background : Antibiotic resistance emerges as a major issue for Helicobacter pylori (H. pylori) treatment. High-dose dual therapy has recently shown encouraging results in H. pylori eradication, but it has yet to be validated in this H. pylori highly infected area; it is also not known if this concept can be extended to antibiotics other than amoxicillin, and factors that affect the eradication. We investigate if rabeprazole plus amoxicillin or furazolidone regimens could be a first-line therapy for H. pylori eradication, and factors that affect the curing rate. Methods : This is a single-center, prospective, open-label, randomized-controlled trial. Naive patients (n=292) were randomly treated with bismuth-containing quadruple therapy (BQT), rabeprazole plus amoxicillin (RADT), or furazolidone (RFDT) groups. RADT and FADT use three times daily regimens. H. pylori diagnosis and eradication were determined and confirmed by ¹³C-urea breath test. Results : In per-protocol (PP) anal., H. pylori eradication rate was 91.2in BQT group, 89.6in RADT, and 51.0in RFDT group. In intention-to-treat (ITT) anal., infection was eradicated in 86.7of patients in BQT group, 85.8in RADT, and 48.1in RFDT groups, resp. Noninferiority was confirmed between BQT and RADT groups. The incidence of side effects in BQT group was significantly higher than that in RADT group. Successful eradication was associated with lower body surface area (BSA) and low body mass index (BMI) in BQT group. Smoking and high BSA index reduced H. pylori eradication rate in RADT group. Conclusions : Rabeprazole-amoxicillin dual therapy is equally effective to the bismuth-containing quadruple therapy for H. pylori eradication with fewer side effects and saves use of one antibiotic per each treatment. Successful eradication is also associated with low BSA and non-smoking condition, which deserves future stratified anal. for refinement and optimization. This study involved multiple reactions and reactants, such as Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6Formula: C18H20N3NaO3S).

Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6) belongs to imidazole derivatives. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole has become an important synthon in the development of new drugs. Imidazole also acts as a microtubule destabilizing agents and inhibits topoisomerase and Cytochrome P450 Family 26 Subfamily A Member 1 (CYP26A1) enzymes.Formula: C18H20N3NaO3S

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Protocol of a randomized, double-blind, placebo-controlled study of the effect of probiotics on the gut microbiome of patients with gastro-oesophageal reflux disease treated with rabeprazole was written by Liu, Wenjun;Xie, Yong;Li, Yingmeng;Zheng, Longjin;Xiao, Qiuping;Zhou, Xu;Li, Qiong;Yang, Ni;Zuo, Kexuan;Xu, Tielong;Lu, Nong-Hua;Zhang, Heping. And the article was included in BMC Gastroenterology in 2022.Computed Properties of C18H20N3NaO3S The following contents are mentioned in the article:

For patients with gastro-oesophageal reflux symptoms, the preferred treatment is proton pump inhibitor (PPI) administration for approx. 8 wk. However, long-term use of PPIs can cause gut microbiome (GM) disturbances. This study is designed to evaluate the effect of probiotics combined with a PPI on the GM and gastrointestinal symptoms of patients with gastro-oesophageal reflux disease (GERD). This is a randomized, double-blind, placebo-controlled trial. A total of 120 eligible patients with GERD will be randomized into the exptl. group or the control group. The treatment includes two phases: the initial treatment period lasts 8 wk (weeks 1-8), and the maintenance treatment period lasts 4 wk (weeks 9-12). During the initial treatment period, the exptl. group will take rabeprazole and LiHuo probiotics, and the control group will take rabeprazole and a probiotic placebo; during the maintenance treatment period, the exptl. group will take LiHuo probiotics, and the control group will take a probiotic placebo. The primary measure is the change in the GM. The secondary measures are the Reflux Disease Questionnaire (RDQ) score, Gastrointestinal Symptom Rating Scale (GSRS) score, faecal metabolome (FM), body mass index, Los Angeles grade of oesophagitis, adverse event (AE) rate and treatment compliance. Each outcome indicator will be assessed at day 0 (before administration), day 28 and/or 56 (during administration), and day 84 (end of administration) to reveal intragroup differences. AEs will be monitored to assess the safety of LiHuo probiotics. This will be the first trial to use the intestinal flora metagene method to analyze the effects of probiotics on patients with GERD receiving long-term PPI treatment. The goal is to provide evidence for the use of probiotics to reduce intestinal flora disorders and other symptoms of gastrointestinal discomfort in patients with GERD who have used PPIs for a long period. This study involved multiple reactions and reactants, such as Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6Computed Properties of C18H20N3NaO3S).

Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6) belongs to imidazole derivatives. 1H-imidazole is an imidazole tautomer which has the migrating hydrogen at position 1. It is a conjugate base of an imidazolium cation. It is a conjugate acid of an imidazolide. It is a tautomer of a 4H-imidazole. Imidazole has been usedin the lysis, wash and elution buffer for the purification of histidine tagged Sonic Hedgehog(shh-N) protein, in elution buffer in stepwise gradient for the purification of histidine tagged aldo keto reductases using nickel affinity chromatography, as a component of homogenization buffer for the purification of phagosomal compartments from dendritic cells.Computed Properties of C18H20N3NaO3S

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Bioequivalence of a Newly Developed Dabigatran Etexilate Tablet Versus the Commercial Capsule and Impact of Rabeprazole-Induced Elevated Gastric pH on Exposure in Healthy Subjects was written by Harada, Akiko;Ikushima, Ippei;Haranaka, Miwa;Yanagihara, Aki;Nakayama, Daisuke. And the article was included in American Journal of Cardiovascular Drugs in 2020.Formula: C18H20N3NaO3S The following contents are mentioned in the article:

Background and Objective: Dabigatran etexilate (DE) is an anticoagulant with proven efficacy and tolerability for stroke prevention in patients with non-valvular atrial fibrillation. For the com. capsule, a complex formulation is used to maintain the acidic microenvironment required for maximal absorption. Consequently, its efficacy and safety are similar with or without concomitant intake of proton-pump inhibitors (PPIs). A simplified DE tablet formulation was developed and tested in two studies. One investigated bioequivalence (BE) of the novel DE tablet vs. the com. DE capsule. The other investigated DE bioavailability (BA) under pretreatment with the PPI rabeprazole and assessed the effect of elevated pH on exposure to dabigatran. Methods: BE of the novel DE tablet vs. the DE capsule was assessed in a randomized two-treatment, four-period, two-sequence crossover study (NCT03070171). The effect of rabeprazole on the BA of the DE tablet was assessed in an open-label, single-arm study (NCT03143166). Both studies were conducted at sites in Japan. Participants were healthy male volunteers, aged ≥ 20-40 years. In the BE study, participants received the DE tablet or capsule (single oral dose, 110 mg); primary endpoints were area under the concentration-time curve from baseline to the last quantifiable data point (AUC_0-tz) and maximum plasma concentration (C_max) of unconjugated dabigatran. In the relative BA study, participants received the DE tablet (single oral dose, 110 mg) with or without rabeprazole pretreatment (once daily for 5 days, 20 mg); primary endpoints were AUC_0-tz and C_max of total dabigatran. Results: In total, 160 participants were randomized in the BE study; 36 participants were enrolled in the BA study. The 90% confidence intervals of geometric mean (gMean) ratios for AUC_0-tz (101.4-116.0%) and C_max (101.8-116.6%) of unconjugated dabigatran were within pre-defined acceptance criteria for BE. In the relative BA study, the gMeans of AUC_0-tz (667 to 192 ng h/mL) and C_max (83.1 to 21.8 ng/mL) were decreased by approx. 70% when the tablet was administered under rabeprazole pretreatment. The reduction in BA was observed at a mean gastric pH of 5.3. Treatment was well tolerated; no deaths, serious adverse events (AEs) or significant AEs were reported in either study. Conclusion: The DE tablet demonstrated BE to the capsule; however, at high gastric pH, BA of the tablet was reduced by approx. 70%, which may lead to reduced efficacy. Data indicate the importance of examining not only BE under standard conditions, but relative BA at elevated gastric pH. Such investigations may avoid the reduced BA at elevated pH that is quite common in the target population (the elderly and/or patients treated with gastric-acid modifying co-medications), and therefore reduce treatment failure with DE. This study involved multiple reactions and reactants, such as Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6Formula: C18H20N3NaO3S).

Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6) belongs to imidazole derivatives. Many natural products, especially alkaloids, contain the imidazole ring. These imidazoles share the 1,3-C3N2 ring but feature varied substituents. Many drugs contain an imidazole ring, such as certain antifungal drugs, the nitroimidazole series of antibiotics, and the sedative midazolam.Formula: C18H20N3NaO3S

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Comparison of Antioxidant Effects of the Proton Pump-Inhibiting Drugs Omeprazole, Esomeprazole, Lansoprazole, Pantoprazole, and Rabeprazole was written by Abed, Mohammed N.;Alassaf, Fawaz A.;Jasim, Mahmood H. M.;Alfahad, Mohanad;Qazzaz, Mohannad E.. And the article was included in Pharmacology in 2020.SDS of cas: 117976-90-6 The following contents are mentioned in the article:

Peptic lesions usually develop when there is an imbalance between aggressive drivers and gastro-protective mediators that guard the lining of the gastrointestinal tract. The most crucial of these mediators are antioxidants, whose loss may predispose to oxidative stress, which is believed to be the main aggravator of several diseases including peptic ulcer. Proton pump inhibitors (PPIs) are drugs that are highly effective and widely used for therapeutic management of peptic disorders through inhibition of gastric acid secretion. In spite of this, oxidative damage may continue to be a major issue that can predispose to future lesions. The present study is designed to explore the possible antioxidant capability of different PPIs, including omeprazole, esomeprazole, lansoprazole, pantoprazole, and rabeprazole, in an aim to suggest an agent that, in addition to its acid-suppression properties, can provide antioxidant profit. The antioxidant activity of different PPIs was evaluated calorimetrically to test the ability of each drug to quench oxygen free radical, using the well-known stable free radical α,α-diphenyl-β-picrylhydrazyl (DPPH), and compared to ascorbic acid (AA; vitamin C). The measurements were performed using a spectrophotometer at 517 nm. All the studied drugs reduced DPPH, but to different extents. However, omeprazole and esomeprazole showed the highest ability to scavenge free radicals (50% inhibitory concentrations [IC₅₀/s] of the percentage for free radical scavenging activity are 18.7 ± 5.7 and 18.7 ± 5.7, resp., and the AA equivalent are 83,772 ± 11,887 and 81,732 ± 8,523 mg AA/100 g, resp.). Conversely, lansoprazole, pantoprazole, and rabeprazole might be having no role in this story (IC₅₀/s of the percentage for free radical scavenging activity are 49.3 ± 3.1, 49 ± 9.4, and 40.7 ± 7.2, resp., and the AA equivalent are 30,458 ± 3,884, 32,222 ± 10,377, and 37,876 ± 8,816 mg AA/100 g, resp.). Thus, omeprazole and esomeprazole may confer a significant dual action in gastrointestinal protection by providing potent antioxidant properties in addition to their major role as acid-suppression agents. However, further studies are essential to elucidate the mechanism behind the difference between the drugs of the same class. This study involved multiple reactions and reactants, such as Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6SDS of cas: 117976-90-6).

Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6) belongs to imidazole derivatives. Imidazole is a heterocyclic compound with a five-membered planar ring. It is amphoteric and highly polar. Imidazole derivatives have antibacterial, antifungal and anticancer functionality. It interacts with DNA and also binds to protein and stops cell division.SDS of cas: 117976-90-6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

The study of intestinal absorption and biodistribution in vivo of proton pump inhibitors was written by Shen, Tianxiang;Jiang, Xindong;Jin, Zhaolei;Ji, Qiuzhi;Li, Chunlong;Li, Qingpo;Long, Hongxin;Qiu, Weigen;Wang, Wei;Hou, Xuemei;You, Jian. And the article was included in European Journal of Pharmaceutics and Biopharmaceutics in 2020.Electric Literature of C18H20N3NaO3S The following contents are mentioned in the article:

The major therapeutic strategy for acid-related gastrointestinal diseases in clinic is to reduce the excretion of gastric acid by oral administration of proton-pump inhibitors (PPIs). However, it is quite a challenge to study the oral absorption behaviors of PPIs considering their extreme instability under gastrointestinal environment. As a result, little information has been reported on PPI oral absorption so far, hindering the further development of PPI-contained oral preparations Here, we first investigated the degradation rate of three representative PPIs, including ilaprazole, ilaprazole sodium and rabeprazole sodium. Then a modified in situ intestine absorption method in rat was established: through the temperature control by the heat exchangers, the perfusate was kept at physiol. temperature only when passing through the intestine while it was maintained at 4°C outside the intestine. Therefore PPIs could maintained sufficiently high stability under proper temperature control. Our data demonstrated that both ilaprazole and ilaprazole sodium exhibited significantly higher absorption efficiency than rabeprazole sodium did through the comparison of their apparent permeability coefficients and steady-state plasma concentrations after perfusion in the duodenum, jejunum, ileum and colon, mainly attributing to their more suitable oil-water partition coefficient The duodenum could be the best site for the oral absorption of PPIs. Ilaprazole outperformed its sodium salt form with its stable absorption behavior in tested four intestinal segments. Furthermore, after i.v. or oral administration, ilaprazole exhibited a longer residence time and a higher accumulation in the stomach than in most of other tissues/organs. However, it was also found that the accumulation was heterogeneous and mainly located in mucosa cells of the stomach. Our further study indicated that there was no significant difference on the oral absorption efficiency of ilaprazole between female and male rats but ilaprazole underwent a faster metabolism in male rats after oral absorption. Our study provided a valuable guidance for the design of oral formulation and the optimization of PPI-contained formulations. This study involved multiple reactions and reactants, such as Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6Electric Literature of C18H20N3NaO3S).

Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6) belongs to imidazole derivatives. Imidazole is a heterocyclic compound with a five-membered planar ring. It is amphoteric and highly polar. The pharmacophore of imidazole exists in bioactive compounds including amino acids, plant growth regulators and therapeutic agents.n increase of the alkyl chain length of the alcohols. Electric Literature of C18H20N3NaO3S

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem