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205678-26-8

中文名稱 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 結構式 205678-26-8 結構式

基本信息

英文別名
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)-

常見問題列表

生物活性
SB-267268 是一種選擇性和非肽性 αvβ3 和 αvβ5 整合素拮抗劑,對人αvβ3,猴 αvβ3 和 人αvβ5 的 Ki 分別為 0.9,0.5 和 0.7 nM。SB-267268 抑制人和小鼠 αvβ3 的 IC50 值為 0.68 和 0.29 nM。SB-267268 降低血管生成和 VEGF 表達。
體外研究

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.

體內(nèi)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%.
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