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Experimental autoimmune encephalomyelitis (EAE) is the most common animal model of multiple sclerosis (MS), a neuroinflammatory and demyelinating disease characterized by multifocal perivascular infiltrates of immune cells. Although EAE is predominantly considered a T helper 1-driven autoimmune disease, mounting evidence suggests that activated dendritic cells (DC), which are the bridge between innate and adaptive immunity, also contribute to its pathogenesis. Sirtuin 6 (SIRT6), a NAD+-dependent deacetylase involved in genome maintenance and in metabolic homeostasis, regulates DC activation, and its pharmacological inhibition could, therefore, play a role in EAE development. The PK study was performed by Medicilon.

Colorectal tumors, in particular, often show dysregulated WNT/¦Â-catenin signalling. G007-LK may be a candidate for use in preclinical trials to determine the efficacy of this drug in preventing growth of WNT dependent tumors. Doses of the tankyrase inhibitor G007-LK shown to be sufficient to inhibit tumor growth are well tolerated by mice within the time frames investigated. Lineage tracing from LGR5+ intestinal stem cells was reduced upon G007-LK treatment, without altering the main morphological characteristics of the intestine. Moreover, mice treated with G007-LK did not experience weight loss, suggesting that the absorptive capacity of the intestine was not negatively impacted. Medicilon Preclinical Research LCC performed the pharmacokinetic studies.

Cetagliptin demonstrates the great potential for treatment with type 2 diabetes patients based on the inhibition of DPP-4, the increase in GLP-1 and insulin, the decrease in glucose, and might be more effective in DPP-4 inhibition than sitagliptin. This study was conducted in a small, selected population of healthy subjects with normoglycaemia. The results suggest that Cetagliptin, at doses ¡Ý50 mg once daily (QD), exhibited minimal accumulation, inhibited plasma DPP-4 activity by >80% over a 24-hour dosing interval, and increased active glucagon-like-1 peptide (GLP-1) levels without producing hypoglycaemia. The active GLP-1 assays were performed by Medicilon Preclinical Research LLC. Generally, Cetagliptin has favourable clinical tolerability and safety.

Heart failure (HF), known as the terminal stage of various cardiovascular diseases, is characterized by poor prognosis and high mortality. JX01 a promising anti-HF drug candidate, showed good pharmacokinetic and safety profiles. JX01 exhibits better cardiomyocyte protective effects than EMPA in vitro. JX01 exhibits lower minimum effective doses than EMPA in vivo. JX01 has good pharmacokinetic properties. Pharmacokinetic studies were commissioned by Medicilon.

?Stroke is one of the most devastating diseases affecting the health and life of human beings. TBN, a novel tetramethylpyrazine derivative armed with a powerful free radical-scavenging nitrone moiety, has been reported to reduce cerebral infarction in rats through multi-functional mechanisms of action. TBN may serve as a promising new clinical candidate for the treatment of ischemic stroke. Six Cynomolgus macaque monkeys were used for pharmacokinetic study. TBN were given intravenously at doses of 30 and 90?mg/kg, 3 monkeys for each dose. TBN (purity 99.3%) used in this study was synthesized by Medicilon.