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- 详细信息
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Firategrast
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
402567-16-2
- 规格：
50mg/25mg/10mg/1mg/5mg
| 规格： | 50mg | 产品价格： | ￥5590.0 |
|---|---|---|---|
| 规格： | 25mg | 产品价格： | ￥3490.0 |
| 规格： | 10mg | 产品价格： | ￥1590.0 |
| 规格： | 1mg | 产品价格： | ￥390.0 |
| 规格： | 5mg | 产品价格： | ￥990.0 |
| 基本信息 | |
| CAS | No.402567-16-2 |
| 中文名称 | 非拉司特 |
| 英文名称 | Firategrast |
| 别名 | SB 683699 |
| 分子式 | C27H27F2NO6 |
| 分子量 | 499.5 |
| 溶解性 | Soluble in DMSO(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| SMILES | CCOCC1=CC(=C(C(=C1)OC)C2=CC=C(C=C2)CC(C(=O)O)NC(=O)C3=C(C=CC=C3F)F)OC |
| InChIKey | YLFZHHDVRSYTKT-NRFANRHFSA-N |
| InChI | InChI=1S/C27H27F2NO6/c1-4-36-15-17-13-22(34-2)24(23(14-17)35-3)18-10-8-16(9-11-18)12-21(27(32)33)30-26(31)25-19(28)6-5-7-20(25)29/h5-11，13-14，21H，4，12，15H2，1-3H3，(H，30，31)(H，32，33)/t21-/m0/s1 |
| PubChem CID | 9935681 |
| 靶点 | Integrin(α4β1/α4β7) |
| 通路 | Cytoskeleton |
| 背景说明 | Firategrast 是一种α4β1/α4β7 整合素拮抗剂。 |
| 生物活性 | Firategrast 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]. |
| 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]. |
| 细胞实验 | 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].Animal Model: Female Wild-type C57BL/6J mice (8-12 weeks) with primary TCL1-tg splenocytes[3]；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. |
| 数据来源文献 | [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. |
| 单位 | 瓶 |
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￥390 - 5590
