High Purity 1415823...

High Purity 1415823-73-2 1415823-73-2 in bulk supply evobrutinib in stock
High Purity 1415823-73-2 1415823-73-2 in bulk supply evobrutinib in stock

High Purity 1415823-73-2 1415823-73-2 in bulk supply evobrutinib in stock

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High Purity 1415823-73-2 1415823-73-2 in bulk supply evobrutinib in stock

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High Purity 1415823-73-2 in bulk supply evobrutinib in stock

Evobrutinib is an inhibitor of Bruton's tyrosine kinase (BTK; IC50 = 8.9 nM).It is selective for BTK over a panel of 233 kinases at 1 μM. It inhibits BTK in peripheral blood mononuclear cells (PBMCs; IC50 = 61 nM). Evobrutinib inhibits B cell activation and proliferation in vitro (IC50s = 18.4 and 10.9 nM, respectively). It inhibits mast cell degranulation in a mouse model of passive cutaneous anaphylaxis when administered at doses of 3.95, 19.8, and 39.5 mg/kg. Evobrutinib (1 and 3 mg/kg) reduces cartilage destruction in a rat model of collagen-induced arthritis. It also decreases proteinuria, interstitial inflammation, and the number of glomerular lesions and preserves kidney function in a mouse model of systemic lupus erythematosus (SLE).

Evobrutinib is an inhibitor of Bruton's tyrosin kinase (Btk) inhibitor extracted from patent US20140162983 example 0174.

Evobrutinib can inhibit the activity of BTK and prevent the activation of the BCR signaling pathway. It is metabolized via hydroxylation, hydrolysis, O-dealkylation, glucuronidation, and GSH conjugation.

Details:

Catalogue Number E947503
Chemical Name Evobrutinib
Synonyms 1-(4-(((6-amino-5-(4-phenoxyphenyl)pyrimidin-4-yl)amino)methyl)piperidin-1-yl)prop-2-en-1-one; M-2951;MSC-2364447C
CAS Number 1415823-73-2
Molecular Formula C??H??N?O?
Appearance White to Off-White Solid
Melting Point 173 - 174ºC
Molecular Weight 429.51
Storage Hygroscopic, -20°C Freezer, Under inert atmosphere
Solubility DMSO (Slightly), Methanol (Slightly)
Stability Hygroscopic
Category Standards; Enzyme Activators and Inhibitors;
Applications Evobrutinib is a highly selective inhibitor of the Bruton’s tyrosine kinase (BTK), which is important in the ­development and functioning of various immune cells including B ­lymphocytes and macrophages. Preclinical research suggests it may be therapeutically useful in certain autoimmune diseases.

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