205678-26-8

中文名称 1H-2-Benzazepine-4-acetic acid, 2,3,4,5-tetrahydro-3-oxo-8-[3-(2-pyridinylamino)propoxy]-2-(2,2,2-trifluoroethyl)-, (4S)-

英文名称 1H-2-Benzazepine-4-acetic acid, 2,3,4,5-tetrahydro-3-oxo-8-[3-(2-pyridinylamino)propoxy]-2-(2,2,2-trifluoroethyl)-, (4S)-

CAS 205678-26-8

分子式 C22H24F3N3O4

分子量 451.44

MOL 文件 205678-26-8.mol

205678-26-8 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

化合物 T16851
化合物 SB-267268

英文别名

SB-267268
1H-2-Benzazepine-4-acetic acid, 2,3,4,5-tetrahydro-3-oxo-8-[3-(2-pyridinylamino)propoxy]-2-(2,2,2-trifluoroethyl)-, (4S)-

物理化学性质

沸点677.2±55.0 °C(Predicted)

密度1.320±0.06 g/cm3(Predicted)

酸度系数(pKa)4.32±0.10(Predicted)

形态Solid

颜色White to off-white

常见问题列表

生物活性

SB-267268 是一种选择性和非肽性 αvβ3 和 αvβ5 整合素拮抗剂，对人αvβ3，猴 αvβ3 和人αvβ5 的 Ki 分别为 0.9，0.5 和 0.7 nM。SB-267268 抑制人和小鼠 αvβ3 的 IC50 值为 0.68 和 0.29 nM。SB-267268 降低血管生成和 VEGF 表达。

体外研究

SB-267268 was much less potent for inhibition of human, mouse, and ratαvβ6 integrin. SB-267268 inhibits the attachment of bothαvβ3-transfected HEK293 cells to microtiter plate wells precoated with arginine-glycine-aspartic acid (RGD)-containing matrix proteins with IC ₅₀ values of 12 nM. SB-267268 also inhibits vitronectin-mediated human and rat aortic smooth-muscle-cell (SMC) migration with IC ₅₀ values of approximately 12.3 nM and 3.6 nM, respectively.

体内研究

SB-267268 (60 mg/kg; bi-daily, i.p.) reduces blood vessel profiles (BVPs) in the inner retina by 50%.
In ROP mice treated with SB-267268, VEGF and VEGFR-2 gene expression in the inner nuclear layer (INL) and the ganglion cell layer (GCL) is reduced.

Animal Model:	Pregnant female C57BL/6 mice (ROP mice)
Dosage:	60 mg/kg
Administration:	I.p.; bi-daily
Result:	Reduced blood vessel profiles (BVPs) in the inner retina by 50%.