Search results for: Amantadine-d15 Hydrochloride C10H3D15ClN CAS:
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Controlled drug delivery for glaucoma therapy using montmorillonite/Eudragit microspheres as an ion-exchange carrier.Glaucoma is a serious eye disease that can lead to loss of vision. Unfortunately, effective treatments are limited by poor bioavailability of antiglaucoma medicine due to short residence time on the preocular surface.
2609 related Products with: Controlled drug delivery for glaucoma therapy using montmorillonite/Eudragit microspheres as an ion-exchange carrier.Cultrex In Vitro Angiogen Endothelial Tube Formatio MOUSE ANTI BOVINE ROTAVIR anti CD16 monoclonal anti Astrovirus antibody, Mono Annexin V FITC Reagent Annexin V FITC Reagent100 Annexin V FITC Reagent Annexin V FITC Reagent200 Annexin V Cy3 Reagent Annexin V Cy3 Reagent1000 Annexin V Cy3 Reagent
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Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect.In the present study, a series of multi-target N-substituted cyclic imide derivatives which possessed potent dopamine D, serotonin 5-HTand 5-HTreceptors properties were synthesized and evaluated as potential antipsychotics. Among these compounds, (3aR,4R,7S,7aS)-2-(4-(4-(benzo[b]thiophen-4-yl)piperazin-1-yl)butyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione hydrochloride (3d) held a promising pharmacological profile. 3d not only showed potent and balanced in vitro activities on D/5-HT/5-HTreceptors, but also endowed with low to moderate activities on 5-HT, H, α, Mreceptors and hERG channel, suggesting a low liability to induce side effects such as weight gain, orthostatic hypotension and QT prolongation. In animal behavioral studies, 3d reduced phencyclidine-induced hyperlocomotion with a high threshold for catalepsy induction. Compound 3d was selected as a potential antipsychotic candidate for further development.
2002 related Products with: Synthesis and biological evaluation of a series of multi-target N-substituted cyclic imide derivatives with potential antipsychotic effect.MOUSE ANTI BOVINE ROTAVIR Androgen Receptor (Phosph Androgen Receptor (Phosph Rabbit Anti-Human Androge Rabbit Anti-Human Androge MOUSE ANTI BORRELIA BURGD RANK Ligand Soluble, Huma RANK Ligand Soluble, Huma Androgen Receptor (Ab 650 Cell Meter™ JC 10 Mitoc Cell Meter™ JC 10 Mitoc Cell Meter™ NIR Mitocho
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Histone demethylase LSD1 restricts influenza A virus infection by erasing IFITM3-K88 monomethylation.The histone demethylase LSD1 has been known as a key transcriptional coactivator for DNA viruses such as herpes virus. Inhibition of LSD1 was found to block viral genome transcription and lytic replication of DNA viruses. However, RNA virus genomes do not rely on chromatin structure and histone association, and the role of demethylase activity of LSD1 in RNA virus infections is not anticipated. Here, we identify that, contrary to its role in enhancing DNA virus replication, LSD1 limits RNA virus replication by demethylating and activating IFITM3 which is a host restriction factor for many RNA viruses. We have found that LSD1 is recruited to demethylate IFITM3 at position K88 under IFNα treatment. However, infection by either Vesicular Stomatitis Virus (VSV) or Influenza A Virus (IAV) triggers methylation of IFITM3 by promoting its disassociation from LSD1. Accordingly, inhibition of the enzymatic activity of LSD1 by Trans-2-phenylcyclopropylamine hydrochloride (TCP) increases IFITM3 monomethylation which leads to more severe disease outcomes in IAV-infected mice. In summary, our findings highlight the opposite role of LSD1 in fighting RNA viruses comparing to DNA viruses infection. Our data suggest that the demethylation of IFITM3 by LSD1 is beneficial for the host to fight against RNA virus infection.
1896 related Products with: Histone demethylase LSD1 restricts influenza A virus infection by erasing IFITM3-K88 monomethylation.HA (Influenza A Virus Hem Avian Influenza virus (H7 Recombinant Hemagglutinin Mouse AntiInfluenza B Nuc Goat Anti-Influenza A Vir Goat Anti-Influenza A Vir Goat Anti-Influenza A Vir Mouse Anti-Influenza A Vi Mouse Anti-Influenza A Vi Mouse Anti-Influenza A Vi Goat Anti-Influenza A Vir Rabbit Anti-Influenza A V
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Novel Vilazodone-Tacrine Hybrids as Potential Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease Accompanied with Depression: Design, Synthesis, and Biological Evaluation.Depression is one of the most frequent psychiatric complications of Alzheimer's disease (AD), affecting up to 50% of the patients. A novel series of hybrid molecules were designed and synthesized by combining the pharmacophoric features of vilazodone and tacrine as potential multitarget-directed ligands for the treatment of AD with depression. In vitro biological assays were conducted to evaluate the compounds; among the 30 hybrids, compound 1e showed relatively balanced profiles between acetylcholinesterase inhibition (IC= 3.319 ± 0.708 μM), 5-HTagonist (EC= 107 ± 37 nM), and 5-HT reuptake inhibition (IC= 76.3 ± 33 nM). Compound 1e displayed tolerable hepatotoxicity and moderate hERG inhibition activity, and could penetrate the blood-brain barrier in vivo. Furthermore, an oral intake of 30 mg/kg 1e·HCl could significantly improve the cognitive function of scopolamine-induced amnesia mice and alleviate the depressive symptom in tail suspension test. The effectivity of 1e validates the rationality of our design strategy.
1155 related Products with: Novel Vilazodone-Tacrine Hybrids as Potential Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease Accompanied with Depression: Design, Synthesis, and Biological Evaluation.Beta Amyloid (42) ELISA K Beta Amyloid (1 40) ELISA Beta Amyloid (40) ELISA K Beta Amyloid (1 40) ELISA Glucose Assay With the La Directed In Vivo Angiogen Screen Quest™ Membrane Screen Quest™ Membrane Screen Quest™ Membrane Screen Quest™ Membrane ENZYMATIC ASSAY KITS (CH Bovine Androstenedione,AS
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Development of a high-throughput fluorescence polarization assay for the discovery of EZH2-EED interaction inhibitors.Aberrant activity of enhancer of zeste homolog 2 (EZH2) is associated with a wide range of human cancers. The interaction of EZH2 with embryonic ectoderm development (EED) is required for EZH2's catalytic activity. Inhibition of the EZH2-EED complex thus represents a novel strategy for interfering with the oncogenic potentials of EZH2 by targeting both its catalytic and non-catalytic functions. To date, there have been no reported high-throughput screening (HTS) assays for inhibitors acting at the EZH2-EED interface. In this study, we developed a fluorescence polarization (FP)-based HTS system for the discovery of EZH2-EED interaction inhibitors. The tracer peptide sequences, positions of fluorescein labeling, and a variety of physicochemical conditions were optimized. The high Z' factors (>0.9) at a variety of DMSO concentrations suggested that this system is robust and suitable for HTS. The minimal sequence requirement for the EZH2-EED interaction was determined by using this system. A pilot screening of an in-house compound library containing 1600 FDA-approved drugs identified four compounds (apomorphine hydrochloride, oxyphenbutazone, nifedipine and ergonovine maleate) as potential EZH2-EED interaction inhibitors.
2902 related Products with: Development of a high-throughput fluorescence polarization assay for the discovery of EZH2-EED interaction inhibitors.EnzyChrom™ Kinase Assay MarkerGene™ Multiple Dr Peptoid Ligand Assay Deve Amplite™ Fluorimetric G Amplite™ Fluorimetric G Amplite™ Fluorimetric G Amplite™ Fluorimetric G Amplite™ Fluorimetric F Amplite™ Fluorimetric G Amplite™ Fluorimetric M Amplite™ Fluorimetric G Amplite™ Fluorimetric M
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N-Butyl-4-hydroxy-1,8-naphthalimide: A new matrix for small molecule analysis by matrix-assisted laser desorption/ionization mass spectrometry.The matrix plays an essential role in defining detection limits and ionization yields of analytes in matrix-assisted laser desorption/ionization mass spectrometry (MALDI-MS) analysis. Small molecule MALDI-MS analyses commonly suffer from the high background interference generated from matrices. Moreover, the inhomogeneous crystallization of some matrices, such as 2,5-dihydroxybenzoic acid (DHB), is to the detriment of the quality or repeatability of detection. We have found that N-butyl-4-hydroxy-1,8-naphthalimide (BHN) can provide improved performance as a matrix for small molecule analysis.
1973 related Products with: N-Butyl-4-hydroxy-1,8-naphthalimide: A new matrix for small molecule analysis by matrix-assisted laser desorption/ionization mass spectrometry.Mouse Anti-Human Matrix M Mouse Anti-Human Matrix M Mouse Anti-Human Matrix M (3S,4aS,8aS)-2-[(2R,3R)-3 (3R,4S,5R,6S)-1-Aza-4-hyd [(1S,2R)-1-Benzyl-2-hydro [(1S,2R)-1-Benzyl-2-hydro [(1S,2R)-1-Benzyl-2-hydro N-Benzyloxycarbonyl-4-[(3 Rat Anti-Human Cartilage Mouse Anti-Human Fibronec Mouse Anti-Influenza B Ma
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Cytochrome P450 3A selectively affects the pharmacokinetic interaction between erlotinib and docetaxel in rats.Erlotinib as a first-line drug is used in non-small cell lung cancer (NSCLC) patients with sensitive EGFR mutations, while resistance to this drug will occur after several years of treatment. Therefore, the microtubule disturber docetaxel is introduced as combined regimen in clinical trials. This report investigated the potentials and mechanisms of drug-drug interaction (DDI) between erlotinib and docetaxel using wild type (WT) and Cyp3a1/2 knockout (KO) rats. The erlotinib O-demethylation and docetaxel hydroxylation reactions in the absence or the presence of another drug were analyzed in vitro via the assay of rat liver microsomes. In whole animal studies, erlotinib and docetaxel were given to WT and KO rats individually or jointly, and the pharmacokinetic profiles of these two drugs were analyzed and compared among different groups. The results showed that docetaxel not only inhibited the CYP3A-mediated biotransformation of erlotinib in vitro, but also significantly increased the maximum concentration and systemic exposure of erlotinib in vivo in WT rats. In contrast, the DDI was significantly attenuated in KO rats. On the other hand, erlotinib did not influence docetaxel either in vitro biotransformation or in vivo pharmacokinetic behaviors. These results exhibited the potentials of erlotinib-docetaxel interaction and indicated that the CYP3A played the perpetrating role of docetaxel on erlotinib in rats. A better understanding of this DDI with CYP3A may help the regulation of the use of these two drugs, avoid potential problems, and adjust dose carefully and early in clinic.
2415 related Products with: Cytochrome P450 3A selectively affects the pharmacokinetic interaction between erlotinib and docetaxel in rats.Cytochrome P450 3A4 ELISA kit 4-nitrophenol 2 Cytochrome P450 2C9 Cytochrome P450 4A11 anti Cytochrome P450 Antibody Cytochrome P450 Blocking Proteinase Inhibitor 6 (P Thermal Shaker with cooli Human Cytochrome P450 2D6 PTK2 & FLT1 Protein Prote CRKL & SOS1 Protein Prote CRKL & EGFR Protein Prote
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Acetamide Derivatives of Chromen-2-ones as Potent Cholinesterase Inhibitors.Alzheimer's disease (AD), a neurodegenerative disorder, is a serious medical issue worldwide with drastic social consequences. Inhibition of cholinesterase is one of the rational and effective approaches to retard the symptoms of AD and, hence, consistent efforts are being made to develop efficient anti-cholinesterase agents. In pursuit of this, a series of 19 acetamide derivatives of chromen-2-ones were synthesized and evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory potential. All the synthesized compounds exhibited significant anti-AChE and anti-BChE activity, with ICvalues in the range of 0.24-10.19 μM and 0.64-30.08 μM, respectively, using donepezil hydrochloride as the standard. Out of 19 compounds screened, 3 compounds, viz. 22, 40, and 43, caused 50% inhibition of AChE at 0.24, 0.25, and 0.25 μM, respectively. A kinetic study revealed them to be mixed-type inhibitors, binding with both the CAS and PAS sites of AChE. The above-selected compounds were found to be effective inhibitors of AChE-induced and self-mediated Aβaggregation. ADMET predictions demonstrated that these compounds may possess suitable blood-brain barrier (BBB) permeability. Hemolytic assay results revealed that these compounds did not lyse human RBCs up to a thousand times of their ICvalue. MTT assays performed for the shortlisted compounds showed them to be negligibly toxic after 24 h of treatment with the SH-SY5Y neuroblastoma cells. These results provide insights for further optimization of the scaffolds for designing the next generation of compounds as lead cholinesterase inhibitors.
1998 related Products with: Acetamide Derivatives of Chromen-2-ones as Potent Cholinesterase Inhibitors.Cell Meter™ JC 10 Mitoc Cell Meter™ JC 10 Mitoc Cell Meter™ NIR Mitocho Cell Meter™ NIR Mitocho Cell Meter™ Mitochondri Screen Quest™ Membrane Screen Quest™ Membrane Screen Quest™ Membrane Screen Quest™ Membrane EnzyChrom™ Kinase Assay Rapid Microplate Assay K Astra Blue Solution
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Protein digestomic analysis reveals the bioactivity of deer antler velvet in simulated gastrointestinal digestion.Proteins are the most prominent bioactive component in deer antler velvet. The aim of the present study was to track the fate of protein of antler velvet by protein digestomics. The peptide profile identified by LC-MS/MS and the in vitro bioactivity of antler velvet aqueous extract (AAE) were investigated in simulated gastrointestinal digestion. A total of 23, 387 and 417 peptides in AAE, gastric and pancreatic digests were identified using LC-MS/MS, respectively. Collagens, the predominant proteins, released 34 peptides in gastric digests and 146 peptides in pancreatic digests. The gastric and pancreatic digests presented dipeptidyl peptidase IV (DPP-IV) and prolyl endopeptidase (PEP) inhibition activities. Four peptides from digests were proved to be DPP-IV and PEP inhibitory peptides. The results showed that the peptides released from antler velvet protein contributed to the bioactivity of antler velvet during digestion.
1665 related Products with: Protein digestomic analysis reveals the bioactivity of deer antler velvet in simulated gastrointestinal digestion.HIV 1 intergase antigen. Human Macrophage Inflamma Human Macrophage Inflamma Human Macrophage Inflamma Human Macrophage Inflamma Human Macrophage Inflamma Human Gro g Macrophage In Mouse Macrophage Inflamma Mouse Macrophage Inflamma Mouse Macrophage Inflamma Mouse Macrophage Inflamma Native Influenza HA (A Br
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Imaging-guided synergetic therapy of orthotopic transplantation tumor by superselectively arterial administration of microwave-induced microcapsules.It is an ambitious target to improve overall Hepatocellular Carcinoma therapeutic effects. Recently, MW ablation has emerged as a powerful thermal ablation technique, affording favorable survival with excellent local tumor control. To achieve better therapeutic effects of MW ablation, MW sensitizers are prepared for enhanced MW ablation to preferentially heat tumor territory. However, it is still not practicable for treatment of the orthotopic transplantation tumor. Herein, biocompatible and degradable methoxy poly(ethylene glycol)-poly(lactic-co-glycolic acid) (mPEG-PLGA) microcapsules with hierarchical structure have been designed for microwave-induced tumor therapy. Chemical drug doxorubicin hydrochloride (DOX·HCl), microwave (MW) sensitizers and CT imaging contrast MoSnanosheets and MR imaging contrast FeOnanoparticles are co-incorporated into the microcapsules. In vitro/vivo MR/CT dual-modal imaging results prove the potential application for guiding synergetic therapy and predicting post-therapy tumor progression in the orthotopic transplantation tumor model. After blocking the tumor-feeding arteries, these microcapsules not only exclude the cooling effect by cutting off the blood flow but also enhance MW heating conversion at tumor site. The focused MW heating makes microcapsules mollescent or ruptured and releases DOX·HCl from the microcapsules, achieving the controlled release of drugs for chemical therapy. Compared with MW ablation, 29.4% increase of necrosis diameter of normal liver in rabbit is obtained under MW ablation combined with transcatheter arterial blocking, and the average size of necrosis and inhibition rate of VX-2 liver orthotopic transplantation tumor in rabbit has increased by 129.33% and 73.46%. Moreover, it is proved that the superselectively arterial administration of the as-prepared microcapsules has no recognizable toxicity on the animals. Therefore, this research provides a novel strategy for the construction of MW-induced microcapsules for orthotopic transplantation tumor ablation with the properties of MW sensitizing, superselective arterial blocking, control release and enhanced accumulation of DOX·HCl, and MR/CT dual-modal imaging, which exhibits great potential applications in the field of HCC therapy.
2023 related Products with: Imaging-guided synergetic therapy of orthotopic transplantation tumor by superselectively arterial administration of microwave-induced microcapsules.Ofloxacin CAS Number [824 Copper Stain Kit (For Mi Copper Stain Kit (For Mi ELISA Kit for Tumor Necr PolyTek HRP Anti-Rabbit PolyTek HRP Anti-Mouse P PTAH Stain Kit for Micro PTAH Stain Kit for Micro Anti AGO2 Human, Monoclon Anti AGO2 Mouse, Monoclon Anti AGO2 Human, Monoclon Anti AGO2 Mouse, Monoclon
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