Firategrast|402567-16-2|-陌孚医药/Medlife

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Firategrast

目录号: PL14856 纯度: ≥99%

CAS No. :402567-16-2

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中文名称	Firategrast
中文别名	Firategrast（SB683699）抑制剂;非拉司特;Firategrast
英文名称	Firategrast
英文别名	[1,1'-Biphenyl]-4-propanoic acid, α-[(2,6-difluorobenzoyl)amino]-4'-(ethoxymethyl)-2',6'-dimethoxy-, (αS)-;Firategrast;SB 683699;(2S)-2-[(2,6-difluorobenzoyl)amino]-3-[4-[4-(ethoxymethyl)-2,6-dimethoxyphenyl]phenyl]propanoic acid;SB-683699;(alphaS)-alpha-[(2,6-Difluorobenzoyl)amino]-4'-(ethoxymethyl)-2',6'-dimethoxy-[1,1'-biphenyl]-4-propanoic acid
Cas No.	402567-16-2
分子式	C₂₇H₂₇NO₆F₂
分子量	499.50
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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。

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.

性状

Solid

IC50 & Target[1][2]

α4β1 α4β7

体外研究(In Vitro)

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).
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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.
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (200.20 mM)Ethanol : ≥ 50 mg/mL (100.10 mM)

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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