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Firategrast(SB-683699)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Firategrast(SB-683699)图片
CAS NO:402567-16-2
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 499.5
Formula C27H27F2NO6
CAS No. 402567-16-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: ≥ 100 mg/mL
Water: N/A
Ethanol: N/A
SMILES Code O=C(O)[C@@H](NC(C1=C(F)C=CC=C1F)=O)CC2=CC=C(C3=C(OC)C=C(COCC)C=C3OC)C=C2
Synonyms T-0047; SB 683699; T 0047; SB-683699; T0047; SB683699; Firategrast
实验参考方法
In Vitro

In vitro activity: Firategrast (formerly known as SB-683699 or T-0047) is an orally available alpha4 beta1/alpha4 beta7 (α4β1/α4β7) integrin antagonist designed to reduce trafficking of lymphocytes into the central nervous system (CNS). This could decrease multiple sclerosis (MS) activity, but may compromise CNS immune surveillance. Firategrast treatment was associated with modest decreases in median CSF total, CD4, CD8 and CD19 lymphocyte counts. The generally small magnitude of decreases suggests that sufficient numbers of lymphocytes can access the subarachnoid space, preserving CNS immune surveillance.


Cell Assay: Firategrast is an orally bioavailable α4β1/α4β7 integrin antagonist designed to reduce trafficking of lymphocytes into the central nervous system (CNS). Median (n, range) CSF lymphocyte counts (cells/μl) at weeks 0, 24, 28 and 36 were: 5.3 (44, 0.3-70.2), 3.3 (31, 0.0-99.0), 3.0 (32, 0.0-58.2) and 3.5 (29, 0.0-274.8). CD4+, CD8+ T- and CD19+ B-lymphocyte counts followed a similar pattern. Minimal changes were observed for CD3-CD16+CD56+ natural killer cells. Median CD4 : CD8 ratios were: 2.9 (41, 1.1-10.9), 2.2 (29, 0.6-5.9), 3.8 (28, 1.6-9.0) and 3.8 (21, 2.1-9.4). Blood lymphocyte counts were elevated at weeks 4 and 24, consistent with the mechanism of firategrast, and returned to baseline when firategrast was discontinued. There were minimal changes in CD4 : CD8 ratios.

In Vivo Forty-six subjects with relapsing forms of MS were treated for up to 24 weeks with open-label firategrast, 900 (females) or 1200 (males) mg twice daily. CSF and blood cell counts, and lymphocyte composition were determined using flow cytometry.
Animal modelNA
Formulation & DosageNA
References Eur J Neurol. 2013 Jul;20(7):1032-42