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SB273005
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。
SB273005图片
CAS NO:205678-31-5
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)451.44
FormulaC22H24F3N3O4
CAS No.205678-31-5
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 90 mg/mL (199.4 mM)
Water: <1 mg/mL
Ethanol: 16 mg/mL (35.4 mM)
Other infoChemical Name: 2-[(4S)-8-[2-[6-(Methylamino)pyridin-2-yl]ethoxy]-3-oxo-2-(2,2,2-trifluoroethyl)-4,5-dihydro-1H-2-benzazepin-4-yl]acetic acid
InChi Key: KSSPHFGIOASRDE-HNNXBMFYSA-N
InChi Code: InChI=1S/C22H24F3N3O4/c1-26-19-4-2-3-17(27-19)7-8-32-18-6-5-14-9-15(11-20(29)30)21(31)28(12-16(14)10-18)13-22(23,24)25/h2-6,10,15H,7-9,11-13H2,1H3,(H,26,27)(H,29,30)/t15-/m0/s1
SMILES Code: O=C(O)C[C@H]1C(N(CC(F)(F)F)CC2=CC(OCCC3=NC(NC)=CC=C3)=CC=C2C1)=O
SynonymsSB-273005; SB 273005; SB273005
实验参考方法
In Vitro

In vitro activity: In vitro, SB273005 inhibits human osteoclast-mediated bone resorption with IC50 of 11 nM. In blood containing MDA-MB-231 cells, a combination of SB273005 and lamifiban inhibits tumor cell adhesion to vascular extracellular matrix (ECM).


Kinase Assay: SB 273005 binds αvβ3 and αvβ5 with low nM affinity, but binds weakly to integrins αIIbβ3 and α5β1. SB 273005 inhibits αvβ3-mediated cell adhesion with an IC50 value of 3 nM, endothelial cell migration with an IC50 of 1.8 nM, and osteoclast-mediated bone resorption with an IC50 of 11 nM in vitro.

In VivoIn rat models of bone resorption and osteoporosis, SB273005 (30 mg/kg, p.o.) inhibits the parathyroid hormone-stimulated calcemic response, and inhibits bone loss. In rat with adjuvant-induced arthritis, SB273005 (60 mg/kg, p.o.) significantly reduces the symptoms of adjuvant-induced arthritis. SB273005 (1000 mg/kg/day, p.o.) causes acute, transient necrosis of vascular smooth muscle cell (VSMC) in aorta and renal arteries of mice. In pregnant mice, SB273005 reverses the reduction of Th1 cell-produced IL-2 levels and the increase of Th2 cell-derived IL-10 levels.
Animal modelThyroidectomized–parathyroidectomized (TPTx) rat model of bone resorption, and ovariectomized (Ovx) rat model of osteoporosis
Formulation & DosageDissolved in 1% methylcellulose; 30 mg/kg; i.p. injection
ReferencesJ Med Chem. 2000 Jan 13;43(1):22-6; Arthritis Rheum. 2001 Jan;44(1):128-37.