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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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Discovery of novel PDE4 inhibitors for the topical treatment of Psoriasis. The metabolic stability on mouse, rat, and human liver microsomes was determined by Medicilon

2023-07-11
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Psoriasis is a common immune-mediated skin disorder manifesting in abnormal skin plaques, and PDE4 is an effective target for the treatment of inflammatory diseases such as psoriasis.

Researchers designed and synthesized the lead compound with high PDE4 inhibitory potency and remarkable metabolite profiles in liver microsomes.

The metabolic stability on mouse, rat, and human liver microsomes was determined by Medicilon.

Reference:

Zhendong Song, et al. Discovery and Structural Optimization of Toddacoumalone Derivatives as Novel PDE4 Inhibitors for the Topical Treatment of Psoriasis. J Med Chem. 2022 Mar 10;65(5):4238-4254. doi: 10.1021/acs.jmedchem.1c02058. 

inflammatorypsoriasismetabolic-stability
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Relevant News
Design, synthesis, and evaluation of potent RIPK1 inhibitors with in vivo anti-inflammatory activity. The PK parameters were determined at Medicilon
2023-07-11
RIPK1 plays a key role in the necroptosis pathway that regulates inflammatory signaling and cell death in various diseases, including inflammatory and neurodegenerative diseases. Herein, researchers report a series of potent RIPK1 inhibitors, represented by compound 70. Compound 70 possesses favorable pharmacokinetic parameters with moderate clearance and good oral bioavailability in SD rat. The pharmacokinetic parameters were determined at Medicilon using male SD rats (3 rats per group, 4 groups).
RIPK2 is an enzyme involved in numerous chronic inflammatory conditions. UH15-15 inhibits RIPK2 kinase and demonstrates favorable in vitro ADME and PK properties. The PK study was conducted by Medicilon
2023-07-11
Receptor interacting protein kinase-2 (RIPK2) is an enzyme involved in the transduction of pro-inflammatory nucleotide-binding oligomerization domain cell signaling, a pathway implicated in numerous chronic inflammatory conditions. UH15-15 inhibits RIPK2 kinase (IC50=8 nM) and demonstrates favorable in vitro ADME and pharmacokinetic properties. The pharmacokinetic study was conducted by Medicilon.
XY153 is a valuable lead compound for the development of potential therapeutics against acute myeloid leukemia. XY153 demonstrated good metabolic stability in vitro. All liver microsome assays were performed by Medicilon
2023-07-17
Pan-bromodomain and extra terminal (Pan-BET) inhibitors show profound efficacy but exhibit pharmacology-driven toxicities in clinical trials. The representative Compound 8l (XY153), a novel BD2-selective BET inhibitor, potently binds to BRD4 BD2 with an IC50 value of 0.79 nM. XY153 displayed potent antiproliferative activity against multiple tumor cell lines. XY153 also demonstrated good metabolic stability in vitro. These data indicate that XY153 may serve as a new and valuable lead compound for the development of potential therapeutics against acute myeloid leukemia (AML). All liver microsome assays were performed by Medicilon.
Stock Code
688202

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Address: 20 Maguire Road, Suite 103, Lexington, MA 02421(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

Tel: +82 70-8269-5849

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Postcode: 201299

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

Fax: +86 (21) 5859-6369

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