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The Shanghai Overseas Returned Scholars Association invites the Dutch PhD delegation to visit Medicilon, exploring paths for innovative development together
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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

2023-07-17
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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.

34.jpgReference:

Wuqiang Wen, et al. N-Acylamino Saccharin as an Emerging Cysteine-Directed Covalent Warhead and Its Application in the Identification of Novel FBPase Inhibitors toward Glucose Reduction. J Med Chem. 2022 Jul 14;65(13):9126-9143. doi: 10.1021/acs.jmedchem.2c00336. 

FBPasediabeteshepatocyte-modelpharmacokinetic-studiespreclinical
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Relevant News
Discovery and preclinical development of orally active and highly selective follicle stimulating hormone receptor agonists. Toxicological evaluations in both rat and dog were performed by Medicilon
2023-07-11
TOP5300 is an orally active follicle stimulating hormone receptor allosteric agonist that provides a preferred treatment for over 16 million infertile women of reproductive age in low complexity methods or in high complexity methods. TOP5300 was evaluated in standard ADME, including Cytochrome P450 inhibition, clearance and pharmacokinetic profiles. Toxicological evaluations were performed in both rat and dog as the second species according to the guidance from FDA. These assays were performed by Medicilon.
Design and synthesis of selective orally bioavailable threonine tyrosine kinase (TTK) inhibitors. The pharmacokinetic studies were carried out by Medicilon
2023-07-11
Threonine tyrosine kinase (TTK), a dual-specificity protein kinase, acts as a core component of the spindle assembly checkpoint and plays a crucial role in accurate separation of sister chromatids during mitosis to avoid aneuploidy. TTK inhibition is an attractive wide-spectrum strategy for cancer therapy. Researchers designed and synthesized a series of pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable TTK inhibitors. All the pharmacokinetic studies were carried out by Medicilon. Compounds 5o exhibits strong binding affinity to TTK with a Kd value of 0.15 nM. Compound 5o demonstrates good oral pharmacokinetic properties.
QF-036 is an HIV-1 maturation inhibitor in preclinical development with favourable pharmacokinetic properties. The pharmacokinetic studies were performed by Medicilon
2023-07-11
QF-036 is an HIV-1 maturation inhibitor in preclinical development. After oral QF-036 administration to rats and monkeys, both species exhibit moderate bioavailability, and the plasma drug exposure increased in an approximately dose-proportional manner. The favourable viral inhibitory activity and pharmacokinetic properties provide critical support for QF-036 as a promising anti-HIV therapeutic candidate. The pharmacokinetic studies were performed by Medicilon.
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Address: 470 Wildwood Ave, Woburn, MA 01801 (America)

Tel: +1(626)986-9880(U.S.)

Address: Allia Future Business Centre Kings Hedges Road Cambridge CB4 2HY, UK

Tel: 0044 7790 816 954 (Europe)

Email: marketing@medicilon.com

  

Address: 5th Floor, 62, Banpodae-ro 4-gil, Seocho-gu, Seoul, 06719 South Korea

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Postcode: 201299

Tel: +86 (21) 5859-1500 (main line)

Fax: +86 (21) 5859-6369

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