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MedChemExpress - Model Zabedosertib - ...

MedChemExpress - Model Zabedosertib - 1931994-81-8

Zabedosertib (BAY 1834845) is a selective, orally active IRAK4 inhibitor with immunomodulatory potential, IC50 is 3.55 nM. IRAK4 is a protein kinase involved in signaling innate immune responses from Toll-like receptors[1]. Zabedosertib exhibits anti-inflammatory property against IL-β, LPS (HY-D1056) and Imiquimod (HY-B1080) induced inflammation[2].

Zabedosertib

MCE China：Zabedosertib

Brand：MedChemExpress (MCE)

Cat. No.HY-139374

CAS：1931994-81-8

Synonyms：BAY 1834845

Purity：98.14%

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：Zabedosertib (BAY 1834845) is a selective, orally active IRAK4 inhibitor with immunomodulatory potential, IC50 is 3.55 nM. IRAK4 is a protein kinase involved in signaling innate immune responses from Toll-like receptors. Zabedosertib exhibits anti-inflammatory property against IL-β, LPS (HY-D1056) and Imiquimod (HY-B1080) induced inflammation.

In Vitro：Zabedosertib decreases inflammatory cytokines secretion (500 nM), such as IL-1, IFN-γ, TNF-α, and IL-17[2].

In Vivo：Zabedosertib (150 mg/kg, p.o., twice) prevents lung injury and reduces inflammation in LPS induced ARDS in BALB/c mice[2]. Zabedosertib inhibits IL-β(p.o., 40-80 mg/kg, once), LPS (p.o., 10-40 mg/kg, once) and Imiquimod (p.o., 15-150 mg/kg, twice daily for 7 days) induced inflammation[3]. Zabedosertib has a Pharmacokinetic profile in rats[3]: Pharmacokinetic Analysis of Zabedosertib in rats[1] species Doseiv (mg/kg) AUCnorm,iv (kg·h/L) CLblood (L/h/kg) Vss (L/kg) T1/2,iv (h) Dosepo(mg/kg) AUCnorm,po (kg·h/L)) Cmax,norm (kg/L) Tmax (h) F (%) rat 0.5 5.6 0.24 0.92 4.2 2.0 5.3 0.55 4.0 94 dog 0.5 15 0.088 1.6 17 1.0 15 0.57 2.0 104

IC50 & Target：IRAK4 3.55 nM (IC50)

References：

[1]. Bothe, Ulrich; Siebenreicher, Holger; Schmidt, Nicole; Nubbemeyer, Reinhard; Boemer, Ulf; Guenther, Judith; Steuber, Holger; Lange, Martin; Stegmann, Christian; Sutter, Andreas; et al.New substituted indazoles, methods for the production thereof, pharmaceutical preparations that contain said new substituted indazoles, and use of said new substituted indazoles to produce drugs.WO2016083433A1

[2]. Li Q, et al., Oral IRAK4 inhibitor BAY-1834845 prevents acute respiratory distress syndrome. Biomed Pharmacother. 2022 Sep;153:113459. [Content Brief]

[3]. Bothe U, et al., Discovery of IRAK4 Inhibitors BAY1834845 (Zabedosertib) and BAY1830839. J Med Chem. 2024 Jan 25;67(2):1225-1242. [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。