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Aug 21,2023
TAK-931 is a cancer therapeutic with a unique mechanism of action. Antitumor efficacy studies for TAK-931 were carried out at Medicilon
Replication stress (RS) is a cancer hallmark; chemotherapeutic drugs targeting RS are widely used as treatments for various cancers. To develop next-generation RS-inducing anticancer drugs, cell division cycle 7 (CDC7) has attracted attention as a target. Researchers have developed an oral CDC7-selective inhibitor, TAK-931, as a candidate clinical anticancer drug. TAK-931 demonstrated marked, dose-dependent antitumor activity, without severe body weight loss. Antitumor efficacy studies for TAK-931 were carried out in two pancreatic PDX models, PHTX-249Pa and PHTXM-97Pa, at Medicilon.
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TAK-931 is a cancer therapeutic with a unique mechanism of action. Antitumor efficacy studies for TAK-931 were carried out at Medicilon
Jul 18,2023
Academic literature published using Medicilon selenoamino acid medium products
​Medicilon provide complete sets of M9 selenomethionine (SeMET) medium for IPTG-induced E.coli expression system, production of selenomethionine-labeled protein and protein crystallography using multi-wavelength anomalous diffraction (MAD).
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Academic literature published using Medicilon selenoamino acid medium products
Jul 17,2023
AP39, a novel mitochondria-targeted H2S donor, was designed and synthesized by Medicilon
​Alzheimer's disease (AD) is the most universal age-related neurodegenerative disease. AP39 is a newly synthesized mitochondrially targeted H2S donor on mitochondrial function. AP39 increases intracellular H2S levels, mainly in mitochondrial regions. AP39 exerts dose-dependent effects on mitochondrial activity in APP/PS1 neurons. AP39, a novel mitochondria-targeted H2S donor, was designed and synthesized by Medicilon.
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AP39, a novel mitochondria-targeted H2S donor, was designed and synthesized by Medicilon
Jul 17,2023
Discovery of a highly selective and H435R-sensitive thyroid hormone receptor β agonist. PK properties of the TRβ agonist were analyzed by Medicilon.
Thyroid hormone receptors (TRs) are ligand-dependent transcription factors that belong to the nuclear receptor superfamily and also participate in important physiological functions. In this study, Compound 16g is a well-characterized selective and mutation-sensitive TRβ agonist for further investigating its function in treating dyslipidemia, nonalcoholic steatohepatitis (NASH), and resistance to thyroid hormone (RTH). Compound 16g showed excellent lipid metabolism, safety, metabolic stability, and pharmacokinetic properties. PK properties of Compound 16g were analyzed by Medicilon.
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Discovery of a highly selective and H435R-sensitive thyroid hormone receptor β agonist. PK properties of the TRβ agonist were analyzed by Medicilon.
Jul 17,2023
Discovery of novel dual RAGE/SERT inhibitors for treatment of Alzheimer's disease and depression. Pharmacokinetic studies were commissioned by Medicilon
Alzheimer's disease (AD) is a progressive and devastating neurodegenerative disorder, characterized by the presence of β-amyloid (Aβ) peptide plaques, neurofibrillary tangles, and neuroinflammation. Receptor for advanced glycation end products (RAGE) belongs to the immunoglobulin superfamily, which functions as a cell surface acceptor for Aβ peptide. RAGE plays an important role in the Aβ-mediated neuronal damage that closely related to the pathogenesis of AD. In this study, Compound 12 showed good dual-target bioactivities against RAGE and SERT in vitro, good liver microsomal stability, and acceptable pharmacokinetic properties. Pharmacokinetic studies were commissioned by Medicilon.
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Discovery of novel dual RAGE/SERT inhibitors for treatment of Alzheimer's disease and depression. Pharmacokinetic studies were commissioned by Medicilon
Jul 17,2023
TRIM24 and BRPF1 are potential therapeutic targets for cancer. Y08624 is a new TRIM24/BRPF1 dual inhibitor with reasonable Caco-2 permeability. Caco-2 permeability assay was performed by Medicilon
TRIM24 (tripartite motif-containing protein 24) and BRPF1 (bromodomain and PHD finger containing protein 1) are epigenetics "readers”and potential therapeutic targets for cancer and other diseases. Y08624 (Compound 20l) is a new TRIM24/BRPF1 dual inhibitor. Y08624 displays reasonable Caco-2 permeability. Caco-2 permeability assay was performed by Medicilon.
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TRIM24 and BRPF1 are potential therapeutic targets for cancer. Y08624 is a new TRIM24/BRPF1 dual inhibitor with reasonable Caco-2 permeability. Caco-2 permeability assay was performed by Medicilon
Jul 17,2023
IAP proteins are attractive cancer therapeutic targets. SM-406 is a potent and orally bioavailable antagonist of the IAPs. PK studies of SM-406 in male SD rats, beagle dogs and NHP were performed by Medicilon
Apoptosis is a cellular process critical to the normal development and homeostasis of multicellular organisms. The inhibitor of apoptosis proteins (IAPs) are a class of key apoptosis regulators. IAP proteins are attractive cancer therapeutic targets. SM-406 (compound 2) is a potent and orally bioavailable antagonist of the IAPs. Pharmacokinetic (PK) studies of SM-406 (compound 2) in male Sprague Dawley rats, beagle dogs and cynomolgus monkeys (non-human primates) were performed by the Division of Pharmacokinetics and Metabolism, Medicilon. SM-406 (compound 2) has an excellent PK profile and good oral bioavailability in each of these four species.
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IAP proteins are attractive cancer therapeutic targets. SM-406 is a potent and orally bioavailable antagonist of the IAPs. PK studies of SM-406 in male SD rats, beagle dogs and NHP were performed by Medicilon
Jul 17,2023
Design, synthesis and biological evaluation of a series of FGFRs-dominant multi-target receptor tyrosine kinase inhibitors for the treatment of gastric cancer. The pharmacokinetic analysis was performed by Medicilon
Gastric cancer is the second most lethal cancer across the world. Compounds 8f, inhibits FGFR1 signaling pathways as well as induces cell apoptosis, is a potential agent for the treatment of gastric cancer. The pharmacokinetical profile (PK) of 8f was tested in SD rats. Compound 8f showed an acceptable half-time of 3 h and displayed moderate maximum concentrations, which is enough to meet the concentration of the compound 8f to exert its efficacy in vivo. The pharmacokinetic analysis was performed by the testing service provided by Medicilon.
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Design, synthesis and biological evaluation of a series of FGFRs-dominant multi-target receptor tyrosine kinase inhibitors for the treatment of gastric cancer. The pharmacokinetic analysis was performed by Medicilon
Jul 17,2023
Epigenetic modification plays a major role in the expression of genetic information. The DNA methyltransferase is an attractive target for tumor chemotherapy
Epigenetic modification, like DNA methylation, plays a major role in the expression of genetic information. The DNA methyltransferases (DNMTs), maintain DNA methylation, is an attractive target for tumor chemotherapy. WK-23 displays a good inhibitory effect on human DNMT1 with an IC50 value of 5.0 µM. The PK profile of WK-23 was obtained with quite satisfying oral bioavailability and elimination half-life. In vivo pharmacokinetic properties of WK-22, WK-23, WK-27, and DC_517 were performed by Medicilon.
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Epigenetic modification plays a major role in the expression of genetic information. The DNA methyltransferase is an attractive target for tumor chemotherapy
Jul 17,2023
FBPase is a promising target associated with cancer and type 2 diabetes. Compounds W8 exhibits high selectivity against FBPase. The pharmacokinetic studies of W8 were performed by Medicilon
Fructose-1,6-bisphosphatase (FBPase) is a promising target associated with cancer and type 2 diabetes. Compounds W8 and W8k exhibit high selectivity against FBPase and W8 effectively reduces blood glucose in an Institute of Cancer Research (ICR) mice model and dose-dependent inhibition of glucose production in a primary mouse hepatocyte model. The pharmacokinetic studies of W8 and its leaving group saccharin were performed by Medicilon.
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FBPase is a promising target associated with cancer and type 2 diabetes. Compounds W8 exhibits high selectivity against FBPase. The pharmacokinetic studies of W8 were performed by Medicilon