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编 号:F349071
分子式:C27H27F2NO6
分子量:499.5
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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生物活性:
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.

体内研究:
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. Animal Model:Female Wild-type C57BL/6J mice (8-12 weeks) with primary TCL1-tg splenocytes
Dosage:30?mg/kg
Administration:Drinking water; daily; starting 2 or 7 days post transplantation to 21 days
Result:Showed an overall reduction of leukemic cells in the spleen, accompanied by significant spleen weight reduction.

体外研究:
Firategrast (0.1-10 μM; 1 hour) significantly reduces chronic lymphocytic leukemia (CLL) cells adhesion. 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).
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