Identification | Back Directory | [Name]
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 | [Synonyms]
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)- | [Molecular Formula]
C22H24F3N3O4 | [MDL Number]
MFCD30533685 | [MOL File]
205678-26-8.mol | [Molecular Weight]
451.44 |
Chemical Properties | Back Directory | [Boiling point ]
677.2±55.0 °C(Predicted) | [density ]
1.320±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
4.32±0.10(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Uses]
SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression[1]. | [in vivo]
SB-267268 (60 mg/kg; bi-daily, i.p.) reduces blood vessel profiles (BVPs) in the inner retina by 50%[1].
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[1]. Animal Model: | Pregnant female C57BL/6 mice (ROP mice)[1] | 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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| [References]
[1] Wilkinson-Berka JL, et al. SB-267268, a nonpeptidic antagonist of alpha(v)beta3 and alpha(v)beta5 integrins, reduces angiogenesis and VEGF expression in a mouse model of retinopathy of prematurity. Invest Ophthalmol Vis Sci. 2006 Apr;47(4):1600-5. DOI:10.1167/iovs.05-1314 |
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