Firategrast

Research use only, not for human use.

Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist that reduces the transport of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity.

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.

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).

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.

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Cell Cycle/DNA Damage

Integrin

Integrin

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402567-16-2

499.5

C27H27F2NO6

>98% (HPLC)

In Vitro:?DMSO : ≥ 100 mg/mL (200.20 mM; ) Ethanol : ≥ 50 mg/mL (100.10 mM)

CCOCc1cc(OC)c(c(OC)c1)-c1ccc(C[C@H](NC(=O)c2c(F)cccc2F)C(O)=O)cc1

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(-20℃)

With Ice Pack

≥ 2 years