Month: November 2022

Wang, Jun-Xia published the artcileLy6G ligation blocks recruitment of neutrophils via a β2-integrin-dependent mechanism, SDS of cas: 321673-30-7, the publication is Blood (2012), 120(7), 1489-1498, database is CAplus and MEDLINE.

Ly6G is a glycosylphosphatidylinositol (GPI)-anchored protein of unknown function that is commonly targeted to induce exptl. neutrophil depletion in mice. In the present study, we found that doses of anti-Ly6G Abs too low to produce sustained neutropenia remained capable of inhibiting exptl. arthritis, leaving joint tissues free of infiltrating neutrophils. Thioglycollate-stimulated peritonitis was also attenuated. No alteration in neutrophil apoptosis was observed, implicating impaired recruitment. Indeed, Ly6G ligation abrogated neutrophil migration toward LTB₄ and other chemoattractants in a transwell system. Exploring the basis for this blockade, we identified colocalization of Ly6G and β2-integrins by confocal microscopy and confirmed close association by both coimmunoprecipitation and fluorescence lifetime imaging microscopy. Anti-Ly6G Ab impaired surface expression of β2-integrins in LTB₄-stimulated neutrophils and mimicked CD11a blockade in inhibiting both ICAM-1 binding and firm adhesion to activated endothelium under flow conditions. Correspondingly, migration of β2-integrin-deficient neutrophils was no longer inhibited by anti-Ly6G. These results demonstrate that exptl. targeting of Ly6G has functional effects on the neutrophil population and identify a previously unappreciated role for Ly6G as a modulator of neutrophil migration to sites of inflammation via a β2-integrin-dependent mechanism.

Blood published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C4H6O3, SDS of cas: 321673-30-7.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Hou, Chunyan published the artcileA hyaluronan-based nanosystem enables combined anti-inflammation of mTOR gene silencing and pharmacotherapy, Quality Control of 1869-45-0, the publication is Carbohydrate Polymers (2018), 339-348, database is CAplus and MEDLINE.

Accompanied by overproduction of oxidants and reduction of pH, inflammation is closely related to many diseases such as cancer, atherosclerosis, and asthma. Besides chemotherapeutic agents, the potential regulative role of autophagy in inflammation is being actively investigated. RNA interference (RNAi)-based gene therapy is widely explored for clin. therapy but seriously restricted by lack of suitable carriers. In this study, we synthesized a hyaluronan-based ROS-sensitive polymer which was expected to release loaded chem. drugs in inflammatory environment and further developed a stable and nontoxic co-delivery nanosystem of siRNA targeting autophagy suppressive gene and chemotherapeutic agents. The in vitro transfection study of this nanosystem revealed improved intracellular accumulation of siRNA and excellent gene silencing efficacy comparable to that of conventional cationic liposome. Moreover, the mRNA expression of inflammatory cytokines was remarkably decreased by our nanosystem. Considering its biocompatibility, transfection efficacy, and anti-inflammatory capability, this co-delivery nanosystem proclaimed to be a promising combined therapeutic strategy for enhanced anti-inflammatory therapy.

Carbohydrate Polymers published new progress about 1869-45-0. 1869-45-0 belongs to amides-buliding-blocks, auxiliary class Trifluoromethylated Building Blocks, name is 2,2,2-Trifluoro-N-(2-mercaptoethyl)acetamide, and the molecular formula is C4H6F3NOS, Quality Control of 1869-45-0.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Dabaeva, V. V. published the artcileSynthesis, Neurotropic Activity, and Molecular Docking of New Condensed Thieno[2,3-b]pyridine Derivatives, SDS of cas: 79-07-2, the publication is Russian Journal of Bioorganic Chemistry (2022), 48(1), 125-134, database is CAplus.

Methods for the preparation of new condensed derivatives of pyrido[3′,2′:4,5]thieno[3,2-d]pyrimidines based on 5,6-dimethyl-2-oxo-1,2-dihydropyridine-3-carbonitrile were developed. Substitution reactions in the 3rd and 4th positions of 7,8-dimethylpyrido[3′,2′:4,5]thieno[3,2-d]pyrimidin-4(3H)-one were conducted. The neurotropic activity of 12 obtained compounds was studied in vivo in rats and mice. Eight compounds were found to have an anticonvulsant effect of antagonism with corazole. Four selected compounds had anxiolytic and behavior activating effects. Mol. docking of the synthesized compounds was performed to predict their interaction with the GABAA receptor. Five compounds were identified, the complexation of which with the GABAA receptor occurs in two places: the benzamidine site of subsite 1 and subsite 3 of the ECD interface, which indicates the inhibitory effect of the compounds on the target.

Russian Journal of Bioorganic Chemistry published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, SDS of cas: 79-07-2.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Dabaeva, V. V. published the artcileSynthesis and Neurotropic Activity of Novel Condensed Cyclopentanopyrido[3′,2′:4,5]-thieno[3,2-D]pyrimidine Derivatives, Recommanded Product: 2-Chloroacetamide, the publication is Pharmaceutical Chemistry Journal (2020), 54(7), 707-713, database is CAplus.

2-Oxo-2,5,6,7-tetrahydro-3-cyano-1H-cyclopenta[b]pyridine was used as the starting point to develop an accessible synthesis of condensed cyclopentanopyrido[3′,2′:4,5]thieno[3,2-d]pyrimidine derivatives I [R = NHNH₂, SC₄H₉, SCH₂CONH₂, etc.] and II [R¹ = C₅H₁₁, CH₂CONH₂, CH₂CH₂OMe, etc.]. The neurotropic activity of these compounds was studied, and a number of them showed anticonvulsant activity as antagonism to corasol. 2-Chloro-6,7-dihydro-5H-cyclepenta[b]pyridine-3-carbonitrile like diazepam, had anti-anxiety and activating effects, while the other compounds had sedative activity.

Pharmaceutical Chemistry Journal published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Recommanded Product: 2-Chloroacetamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Raldua, Demetrio published the artcileBLT-1, a specific inhibitor of the HDL receptor SR-BI, induces a copper-dependent phenotype during zebrafish development, Formula: C12H23N3S, the publication is Toxicology Letters (2007), 175(1-3), 1-7, database is CAplus and MEDLINE.

Block lipid transport-1 (BLT-1) is a small chem. widely used to inhibit the transfer of lipids between high-d. lipoproteins (HDL) and cells mediated by scavenger receptor B, type 1 (SR-BI). This study demonstrated that BLT-1 induced in zebrafish (Danio rerio) embryos a copper-dependent phenotype with a twisted notochord, brain ventricle enlargement, and absence of melanization, phenocopying neocuproine-treated, or calamity mutants. This finding supports an unexpected link between copper availability and SR-BI activity. The copper-chelating activity of BLT-1, revealed by its dramatic effect during embryo development, should be considered in any evaluation of the pharmacol. effect of this thiosemicarbazone derivative on SR-BI activity and the potential therapeutic value of this mol.

Toxicology Letters published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Formula: C12H23N3S.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Nosaka, Takuto published the artcileAlveolar Macrophages Drive Hepatocellular Carcinoma Lung Metastasis by Generating Leukotriene B₄, Category: amides-buliding-blocks, the publication is Journal of Immunology (2018), 200(5), 1839-1852, database is CAplus and MEDLINE.

Macrophages in lungs can be classified into two subpopulations, alveolar macrophages (AMs) and interstitial macrophages (IMs), which reside in the alveolar and interstitial spaces, resp. An i.v. injection of a mouse hepatocellular carcinoma (HCC) cell line, BNL, caused lung metastasis foci with infiltration of AMs and IMs. A 5-lipoxygenase (LOX) inhibitor but not a cyclooxygenase inhibitor reduced the numbers of metastatic foci, particularly those of a larger size. A major 5-LOX metabolite, LTB₄, augmented in vitro cell proliferation of human HCC cell lines as well as BNL cells. Moreover, in this lung metastasis course, AMs exhibited higher expression levels of the 5-LOX and LTB₄ than IMs. Consistently, 5-LOX-expressing AMs increased in the lungs of human HCC patients with lung metastasis, compared with those without lung metastasis. Furthermore, intratracheal clodronate liposome injection selectively depleted AMs but not IMs, together with reduced LTB₄ content and metastatic foci numbers in this lung metastasis process. Finally, IMs in mouse metastatic foci produced CCL2, thereby recruiting blood-borne, CCR2-expressing AMs into lungs. Thus, AMs can be recruited under the guidance of IM-derived CCL2 into metastatic lungs and can eventually contribute to the progression of lung metastasis by providing a potent arachidonic acid-derived tumor growth promoting mediator, LTB₄.

Journal of Immunology published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Category: amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Zingg, Jean-Marc published the artcileα-Tocopheryl Phosphate Induces VEGF Expression via CD36/PI3Kγ in THP-1 Monocytes, SDS of cas: 321673-30-7, the publication is Journal of Cellular Biochemistry (2017), 118(7), 1855-1867, database is CAplus and MEDLINE.

The CD36 scavenger receptor binds several ligands and mediates ligand uptake and ligand-dependent signal transduction and gene expression, events that may involve CD36 internalization. Here we show that CD36 internalization in THP-1 monocytes is triggered by α-tocopherol (αT) and more strongly by α-tocopheryl phosphate (αTP) and EPC-K1, a phosphate diester of αTP and L-ascorbic acid. αTP-triggered CD36 internalization is prevented by the specific covalent inhibitor of selective lipid transport by CD36, sulfo-N-succinimidyl oleate (SSO). Moreover, SSO inhibited the CD36-mediated uptake of 14C-labeled αTP suggesting that αTP binding and internalization of CD36 is involved in cellular αTP uptake, whereas the uptake of αT was less affected. Similar to that, inhibition of selective lipid transport of the SR-BI scavenger receptor resulted mainly in reduction of αTP and not αT uptake. In contrast, uptake of αT was mainly inhibited by Dynasore, an inhibitor of clathrin-mediated endocytosis, suggesting that the differential regulatory effects of αTP and αT on signaling may be influenced by their different routes of uptake. Interestingly, αTP and EPC-K1 also reduced the neutral lipid content of THP-1 cells and the phagocytosis of fluorescent Staphylococcus aureus bioparticles. Moreover, induction of the vascular endothelial growth factor (VEGF) promoter activity by αTP occurred via CD36/PI3Kγ/Akt, as it could be inhibited by specific inhibitors of this pathway (SSO, Wortmannin, AS-605240). These results suggest that αTP activates PI3Kγ/Akt signaling leading to VEGF expression in monocytes after binding to and/or transport by CD36, a receptor known to modulate angiogenesis in response to amyloid beta, oxLDL, and thrombospondin. J. Cell. Biochem. 9999: 1-13, 2017. © 2017 Wiley Periodicals, Inc.

Journal of Cellular Biochemistry published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C5H9IO2, SDS of cas: 321673-30-7.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Hammerman, Ariel published the artcileDapagliflozin Versus Sacubitril-Valsartan to Improve Outcomes of Patients with Reduced Ejection Fraction and Diabetes Mellitus, Quality Control of 137862-53-4, the publication is American Journal of Cardiovascular Drugs (2022), 22(3), 325-331, database is CAplus and MEDLINE.

Abstract: Background: Comorbid heart failure with reduced ejection fraction (HFrEF) and type 2 diabetes mellitus (DM) is associated with a very high risk of HF events. Sacubitril-valsartan, an angiotensin receptor-neprilysin inhibitor (ARNI), and dapagliflozin, a sodium-glucose cotransporter-2 inhibitor, improve HF outcomes in these patients, but their comparative value for money in this patient population has not yet been determined Objective: We aimed to compare the cost needed to treat (CNT) to avoid an HF event with each drug. Methods: CNT was estimated by multiplying the annualized number needed to treat (NNT) to prevent one HF event by the annual cost of each therapy. HF events were defined as the first event of hospitalization for HF or cardiovascular mortality. Drug efficacy data were extracted from published secondary analyses of patients with DM in the DAPA-HF and PARADIGM-HF trials. Drug costs were estimated as 75‰ of the 2021 US National Average Drug Acquisition Cost listing. Sensitivity anal. was performed on parameters that may have affected the CNT. Results: The annualized NNT was 24 (95‰ confidence interval [CI] 16-54) for dapagliflozin and 57 (95‰ CI 31-433) for the ARNI. At an annual cost of $US4523 and 5099, resp., the CNT was $US108,563 (95‰ CI 72,375-244,267) for dapagliflozin and $US290,671 (95‰ CI 158,084-2,208,079) for the ARNI. Conclusions: Dapagliflozin seems to offer greater value for money than the ARNI for patients with HFrEF and DM. Our results provide support for contemporary guidelines advocating the use of dapagliflozin in these patients.

American Journal of Cardiovascular Drugs published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, Quality Control of 137862-53-4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Li, Jiafu published the artcileAre Disinfection Byproducts (DBPs) Formed in My Cup of Tea? Regulated, Priority, and Unknown DBPs, Name: 2-Chloroacetamide, the publication is Environmental Science & Technology (2021), 55(19), 12994-13004, database is CAplus and MEDLINE.

Globally, tea is the second most consumed nonalcoholic beverage next to drinking water and is an important pathway of disinfection byproduct (DBP) exposure. When boiled tap water is used to brew tea, residual chlorine can produce DBPs by the reaction of chlorine with tea compounds In this study, 60 regulated and priority DBPs were measured in Twinings green tea, Earl Gray tea, and Lipton tea that was brewed using tap water or simulated tap water (nanopure water with chlorine). In many cases, measured DBP levels in tea were lower than in the tap water itself due to volatilization and sorption onto tea leaves. DBPs formed by the reaction of residual chlorine with tea precursors contributed ~12% of total DBPs in real tap water brewed tea, with the remaining 88% introduced by the tap water itself. Of that 12%, dichloroacetic acid, trichloroacetic acid, and chloroform were the only contributing DBPs. Total organic halogen in tea nearly doubled relative to tap water, with 96% of the halogenated DBPs unknown. Much of this unknown total organic halogen (TOX) may be high-mol.-weight haloarom. compounds, formed by the reaction of chlorine with polyphenols present in tea leaves. The identification of 15 haloarom. DBPs using gas chromatog.-high-resolution mass spectrometry indicates that this may be the case. Further studies on the identity and formation of these aromatic DBPs should be conducted since haloarom. DBPs can have significant toxicity.

Environmental Science & Technology published new progress about 79-07-2. 79-07-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Aliphatic hydrocarbon chain,Amide,Inhibitor, name is 2-Chloroacetamide, and the molecular formula is C2H4ClNO, Name: 2-Chloroacetamide.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Repova, Kristina published the artcileCardiovascular therapeutics: A new potential for anxiety treatment?, Related Products of amides-buliding-blocks, the publication is Medicinal Research Reviews (2022), 42(3), 1202-1245, database is CAplus and MEDLINE.

A review. Besides the well-recognized risk factors, novel conditions increasing cardiovascular morbidity and mortality are emerging. Undesirable emotions and behavior such as anxiety and depression, appear to participate in worsening cardiovascular pathologies. On the other hand, deteriorating conditions of the heart and vasculature result in disturbed mental and emotional health. The pathophysiol. background of this bidirectional interplay could reside in an inappropriate activation of vegetative neurohormonal and other humoral systems in both cardiovascular and psychol. disturbances. This results in circulus vitiosus potentiating mental and circulatory disorders. Thus, it appears to be of utmost importance to examine the alteration of emotions, cognition, and behavior in cardiovascular patients. In terms of this consideration, recognizing the potential of principal cardiovascular drugs to interact with the mental state in patients with heart or vasculature disturbances is unavoidable, to optimize their therapeutic benefit. In general, beta-blockers, central sympatholytics, ACE inhibitors, ARBs, aldosterone receptor blockers, sacubitril/valsartan, and fibrates are considered to exert anxiolytic effect in animal experiments and clin. settings. Statins and some beta-blockers appear to have an equivocal impact on mood and anxiety and ivabradine expressed neutral psychol. impact. It seems reasonable to suppose that the knowledge of a patient’s mood, cognition, and behavior, along with applying careful consideration of the choice of the particular cardiovascular drug and respecting its potential psychol. benefit or harm might improve the individualized approach to the treatment of cardiovascular disorders.

Medicinal Research Reviews published new progress about 137862-53-4. 137862-53-4 belongs to amides-buliding-blocks, auxiliary class GPCR/G Protein,Angiotensin Receptor, name is (S)-2-(N-((2′-(1H-Tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)pentanamido)-3-methylbutanoic acid, and the molecular formula is C24H29N5O3, Related Products of amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics