Firategrast (SB-683699) is an orally bioavailable alpha4 beta1/alpha4 beta7 integrin antagonist. Firategrast could reduce trafficking of lymphocytes into the central nervous system (CNS). This could decrease multiple sclerosis (MS) activity, but may compromise CNS immune surveillance. The integrins are a sort of transmembrane receptors that modulate the signal transduction from ECM to the cell. They are associated with a lot of diseases such as cancer, inflammation and thrombotic diseases.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 60 mg/mL|
Small Macrocycles As Highly Active Integrin α2β1 Antagonists.
Halland N, et al. ACS Med Chem Lett. 2014 Jan 10;5(2):193-8. PMID: 24900800.
Leukocyte counts in cerebrospinal fluid and blood following firategrast treatment in subjects with relapsing forms of multiple sclerosis.
Grove RA, et al. Eur J Neurol. 2013 Jul;20(7):1032-42. PMID: 23419064.
|Related Integrin Products|
Cilengitide is a potent integrin inhibitor for αvβ3 and αvβ5 receptor with IC50 of 4.1 nM, 79 nM in cell-free assays respectively.
CWHM-12 is a potent inhibitor of αV integrins with IC50 values of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1, respectively.
|Tirofiban hydrochloride monohydrate
Tirofiban hydrochloride monohydrate is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist
Lifitegrast is an integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist; inhibits Jurkat T cell attachment to ICAM-1 with an IC50 of 2.98 nM.
GLPG0187 inhibited the progression of bone metastasis. Maximum efficacy of inhibition of bone metastasis was achieved when GLPG0187 was combined with the standard-of-care metastatic breast cancer treatments.
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