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Home Client Center Publications

SLL-1206 is a kappa opioid receptor agonist with substantially improved physicochemical and pharmacokinetic properties

2023-07-11
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The search for selective kappa opioid receptor (κOR) agonists with an improved safety profile is an area of interest in opioid research. SLL-1206 is a κOR agonist with single-digit nanomolar activities. SLL-1206 exhibits substantially improved physicochemical and pharmacokinetic properties, and reduces central nervous system effects.

The authors are grateful to Medicilon Preclinical Research LLC. for pharmacokinetic studies on SLL-1206.

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Reference:

Qian He, et al. Discovery of an M-Substituted N-Cyclopropylmethyl-7α-phenyl-6,14-endoethanotetrahydronorthebaine as a Selective, Potent, and Orally Active κ-Opioid Receptor Agonist with an Improved Central Nervous System Safety Profile. J Med Chem. 2021 Aug 26;64(16):12414-12433. doi: 10.1021/acs.jmedchem.1c01082. 

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Relevant News
Discovery and synthesis of a new class of selective TNIK inhibitors and evaluation of their anti-colorectal cancer effects, the pharmacokinetic properties was carried out by Medicilon
2023-07-11
The Traf2- and Nck-interacting protein kinase (TNIK) is a downstream signal protein of the Wnt/β-catenin pathway and has been thought of as a potential target for the treatment of colorectal cancer. SAR analysis leads to the identification of a number of potent TNIK inhibitors with Compound 21k being the most active one. Preliminary assessment for the pharmacokinetic properties of Compound 21k was carried out through services provided by Medicilon.
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Idiopathic pulmonary fibrosis is a chronic and lethal lung disease associated with fibroblast activation, myoblast proliferation and extracellular matrix deposition. SKLB-YTH-60 was developed through computer-aided drug design, de novo synthesis and high-throughput screening. YTH-60 has obvious anti‐proliferative activity on fibroblasts and A549 cells. YTH-60 has an acceptable oral bioavailability and appropriate eliminated half-life time. The in vivo pharmacokinetic study of YTH‐60 was performed by Medicilon.
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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

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Fax: +86 (21) 5859-6369

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