Contact Us marketing@medicilon.com
Medicilon Logo
|
search icon search icon 中 contact icon menu icon
Medicilon Logo
|
search icon close search icon 中 contact icon menu icon
ABOUT
Company Profile
Corporate Culture
Management Team
Company History
Message from the CEO
Honors and Awards
Over 20 years of experience in R&D
Learn more
01 Drug Discovery
Chemistry Research
Biology Research
Early Pharmacokinetics
02 Pharmaceutical Research
Intermediates
Active Pharmaceutical Ingredients
Pharmaceutical preparation
Analytical Method Development and Quality Control
CMC Filings
Analytical Testing Center
03 Preclinical Research
Pharmacology & Pharmacodynamics
Drug Safety Evaluation
DMPK
Bioanalysis
IND Filings
01 One-stop Integrated Services
Liposome Drug Development Service Platform
Drug Discovery Platform
Pharmaceutical Research Platform
Preclinical Research Services
Botanical Drug Preclinical R&D Technology Platform
02 Innovative Drug Services
ADC R&D Service Platform
PROTAC R&D Service Platform
mRNA Vaccine Bioanalysis Platform
Non-clinical Research for Cellular Immunotherapies
Nucleic Acid Drug R&D Platform
Peptide Drug Conjugate (PDC) R&D Service Platform
Antibody R&D Service
03 Key Technical Services for Drug R&D
Cytokine and Biomarker Detection Platform
Metabolite Identification (MetID) Service Platform
Drug Forming Research Platform
Flow Cytometry Technology Platform
SEND Format Conversion Platform
Flow Sorting Platform
NanoString nCounter Detection Platform
Routes of Drug Administration Platform
04 Drug Efficacy Evaluation for Common Diseases
IO Pharmacodynamic Model Evaluation Platform
Pharmacodynamic Evaluation Model Platform for Inflammatory and Immune Diseases
Rodent Cerebrovascular Disease Drug Efficacy Evaluation System
05 Advanced Preparation R&D
Inhalation drug R&D platform
Ophthalmic drug R&D platform
Skin Topical Preparation R&D Platform
06 Targeted Drugs R&D Services
STAT3-targeted Drugs R&D Service
GLP-1 New Drug R&D Service
KRAS-targeted Drugs R&D Service
CAREERS
Talent Development
Recruitment
Talent Development
Talent Development
Recruitment
Recruitment
News
Medicilon Events
Featured Stories
Market Events
Videos
A.C.E.
2024-07-22Medicilon Events
The Shanghai Overseas Returned Scholars Association invites the Dutch PhD delegation to visit Medicilon, exploring paths for innovative development together
On July 4th, the Shanghai Overseas Returned Scholars Association invited the Dutch PhD delegation to visit the Chuansha campus of Shanghai Medicilon Inc. (Medicilon) and held discussions with Medicilon's Founder and CEO, Chunlin Chen, among others.
Learn more
2024-07-22Medicilon Events
5th consecutive win! Medicilon once again made the list of "Top 20 Chinese R&D CRO Enterprises in 2024"
Medicilon stood out among hundreds of pharmaceutical enterprises and was honored with the "Top 20 Chinese R&D CRO Enterprises in 2024" award.
Learn more
INVESTORS
Stock Information
Investment Contact
Medicilon 688202
RMB

As of Beijing time The data is from a third-party organization and is only for reference.

For actual information, please refer to：www.eastmoney.com

CLIENT CENTER
Intellectual Property Protection
Clients Testimonials
Downloads
Partnerships
Medicilon Support
Newsletters
U.S.

Address: 470 Wildwood Ave, Woburn, MA 01801 (America)

Tel: +1(626)986-9880

UK

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

Tel: 0044 7790 816 954

Email: marketing@medicilon.com

China

Address: No.585 Chuanda Road, Pudong New Area, Shanghai (Headquarters)

Postcode: 201299

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

Fax: +86 (21) 5859-6369

Close

© 2023 Shanghai Medicilon Inc. All rights reserved Shanghai ICP No.10216606-3

Shanghai Public Network Security File No. 31011502018888 | Website Map

© 2023 Shanghai Medicilon Inc. All rights reserved Shanghai ICP No.10216606-3
Shanghai Public Network Security File No. 31011502018888|Website Map
关闭
中
Message
Contact Us
Close Button
Back To Top
Online Message×
Click switch
Close Button
Customer Center
Customer Center
Case Studies Clients Testimonials Downloads Partnerships Intellectual Property Protection Newsletters
Home Client Center Publications

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
|
Page View：

2.jpg

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
Share：
Return
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

Global

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

Tel: +82 70-8269-5849

China

Address: No.585 Chuanda Road, Pudong New Area, Shanghai (Headquarters)

Postcode: 201299

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

Fax: +86 (21) 5859-6369

Facebook icon
Twitter icon
Linkedin icon
Youtube icon
© 2023 Shanghai Medicilon Inc. All rights reserved All Rights Reserved Privacy Policy
Website Map
-->