MedChemExpress -Model Firategrast -402567-16-2
Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity[1][2][3].MCE products for research use only. We do not sell to patients.
Firategrast
MCE China：Firategrast
Brand：MedChemExpress (MCE)
Cat. No.HY-14951
CAS：402567-16-2
Synonyms：SB 683699
Purity：99.62%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Shipping：Room temperature in continental US; may vary elsewhere.
Description：Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity.
In Vitro：Firategrast (0.1-10 µM; 1 hour) significantly reduces chronic lymphocytic leukemia (CLL) cells adhesion[2]. Firategrast is a potent Integrin α4β1 (VLA-4) antagonist (IC50=198 nM) at inhibiting the binding of soluble VCAM/Fc chimeric protein (sVCAM-1) to G2 acute lymphoblastic leukemia (ALL) cells. VLA-4 is composed of CD49d (α4) and CD29 (β1)[1][4].
In Vivo：Firategrast (30 mg/kg/day in drinking water; starting 2 or 7 days post transplantation to 21 days) shows an overall reduction of leukemic cells in the spleen[3].
IC50 & Target：α4β1 α4β7
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References：
[2]. Sarah E M Herman, et al. Treatment with Ibrutinib Inhibits BTK- and VLA-4-Dependent Adhesion of Chronic Lymphocytic Leukemia Cells In Vivo. Clin Cancer Res. 2015 Oct 15;21(20):4642-51. [Content Brief]
[3]. Eva Szenes, et al. TCL1 transgenic mice as a model for CD49d-high chronic lymphocytic leukemia. Leukemia. 2020 Sep;34(9):2498-2502. [Content Brief]
[4]. H Rahimi, et al. Aberrant regulation of the integrin very late antigen-4 in systemic lupus erythematosus. Lupus. 2013 Mar;22(3):297-306. [Content Brief]
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