产品描述: | 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 |
靶点: |
α4β1;α4β7;Integrin |
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. |
参考文献: |
1. Moses O. Evbuomwan, et al. Generation and Characterization of Novel VLA-4 Inhibitors for Stem Cell Mobilization in Combination with a CXCR2 Agonist. Blood (2017) 130 (Supplement 1): 3197. 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. 3. Eva Szenes, et al. TCL1 transgenic mice as a model for CD49d-high chronic lymphocytic leukemia. Leukemia. 2020 Sep;34(9):2498-2502. 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. |
溶解性: |
Soluble in DMSO、Ethanol |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.002 ml |
10.01 ml |
20.02 ml |
5 mM |
0.4 ml |
2.002 ml |
4.004 ml |
10 mM |
0.2 ml |
1.001 ml |
2.002 ml |
50 mM |
0.04 ml |
0.2 ml |
0.4 ml |
|
注意: |
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