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MedChemExpress - Model RO5461111 - ...

MedChemExpress - Model RO5461111 - 1252637-46-9

RO5461111 a highly specific and orally active antagonist of Cathepsin S with IC50s of 0.4 nM (human Cathepsin S) and 0.5 nM (murine Cathepsin S), respectively. RO5461111 can effectively inhibit the activation of antigen-specific T cells and B cells. RO5461111 can improve pulmonary inflammation and lupus nephritis[1][2].

RO5461111

MCE China：RO5461111

Brand：MedChemExpress (MCE)

Cat. No.HY-114374

CAS：1252637-46-9

Purity：98.17%

Storage：4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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

Description：RO5461111 a highly specific and orally active antagonist of Cathepsin S with IC50s of 0.4 nM (human Cathepsin S) and 0.5 nM (murine Cathepsin S), respectively. RO5461111 can effectively inhibit the activation of antigen-specific T cells and B cells. RO5461111 can improve pulmonary inflammation and lupus nephritis.

In Vitro：RO5461111 (16 h) 在人 (RAJI) 或鼠 (A20) 细胞系中具有细胞活性，显著降低了脾脏树突状细胞的活化以及随后 CD4 T 细胞和 CD4/CD8 双阴性 T 细胞的扩增和活化[1]。

In Vivo：RO5461111 (0.1-100 mg/kg; p.o.; single dose) suppresses T cell priming and antisheep IgG upon vaccination with sheep IgG in BALB/c mice[1]. RO5461111 (1.31 mg/mouse or 30 mg/kg; p.o.; 8 weeks) disrupts germinal centres (as CXCL12) and reduces hypergammaglobulinemia and lupus autoantibody production F in MRL-Fas(lpr) mice. And RO5461111 reduces lung inflammation and improves lupus nephritis[1].

IC50 & Target：human Cathepsin S 0.4 nM (IC50) murine Cathepsin S 0.5 nM (IC50)

References：

[1]. Rupanagudi KV, et al. Cathepsin S inhibition suppresses systemic lupus erythematosus and lupus nephritis because cathepsin S is essential for MHC class II-mediated CD4 T cell and B cell priming. Ann Rheum Dis. 2015 Feb;74(2):452-63. [Content Brief]

[2]. Sanchez RA, et al. Preparation of proline dipeptidyl nitrile derivatives as cathepsin, particularly cathepsin S and L, inhibitors: United States, US20100267722. 2010-10-21.

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。