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MedChemExpress - Model Poseltinib - ...

MedChemExpress - Model Poseltinib - 1353552-97-2

Poseltinib (HM71224) is an orally active, selective, irreversible small molecule Bruton tyrosine kinase (BTK) inhibitor. With an IC50 of 1.95 nM. Poseltinib effectively inhibits the signaling mediated by B cell receptors (BCR), Fc receptors (FcR), and Toll-like receptors (TLR). Poseltinib has anti-inflammatory activity and can be used in the research of rheumatoid arthritis[1][2][3].

Poseltinib

MCE China：Poseltinib

Brand：MedChemExpress (MCE)

Cat. No.HY-109010

CAS：1353552-97-2

Synonyms：HM71224; LY3337641

Purity：98.08%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Poseltinib (HM71224) is an orally active, selective, irreversible small molecule Bruton tyrosine kinase (BTK) inhibitor. With an IC50 of 1.95 nM. Poseltinib effectively inhibits the signaling mediated by B cell receptors (BCR), Fc receptors (FcR), and Toll-like receptors (TLR). Poseltinib has anti-inflammatory activity and can be used in the research of rheumatoid arthritis.

In Vitro：Poseltinib (0.1-100 nM, 30 min) inhibits BCR and FcR signaling in B cells[1]. Poseltinib (1-1000 nM, 1 h) inhibits the phosphorylation of Btk and its downstream molecules such as PLCγ2, in activated Ramos B lymphoma cells in a dose-dependent manner. Inhibits the production of tumor necrosis factor (TNF)-α, interleukin (IL)-6, and IL-1β by human monocytes, and osteoclast formation by human monocytes in primary human B cells [2].BTK, AKT, and PLCγ2 in PBMCs cells[3].

In Vivo：Poseltinib (3,-30 mg/kg, p.o, once a day, from 18 to 40 weeks) reduces the overactivity of B cells by inhibiting BTK, alleviating the development of systemic lupus erythematosus (SLE) and lupus nephritis (LN)[1]. Poseltinib (1-30 mg/kg p.o, once a day for 2 weeks) improves experimental arthritis in mice [2].

IC50 & Target：TLRs

References：

[1]. Kim YY, et al. HM71224, a selective Bruton's tyrosine kinase inhibitor, attenuates the development of murine lupus. Arthritis Res Ther. 2017 Sep 26;19(1):211. [Content Brief]

[2]. Park JK, et al. HM71224, a novel Bruton's tyrosine kinase inhibitor, suppresses B cell and monocyte activation and ameliorates arthritis in a mouse model: a potential drug for rheumatoid arthritis. Arthritis Res Ther. 2016 Apr 18;18:91. [Content Brief]

[3]. Byun JY, et al. Target modulation and pharmacokinetics/pharmacodynamics translation of the BTK inhibitor poseltinib for model-informed phase II dose selection. Sci Rep. 2021 Sep 21;11(1):18671. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。