Firategrast

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Firategrast (SB 683699) 是一种具有口服活性的，特异性的 α4β1/α4β7 整联蛋白拮抗剂。 Firategrast 减少淋巴细胞进入中枢神经系统 (CNS) 的运输，降低多发性硬化症 (MS) 的活性。

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.

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 中的溶解度 : ≥ 100 mg/mL (200.20 mM) Ethanol 中的溶解度 : ≥ 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