| CAS NO: | 205678-31-5 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Molecular Weight (MW) | 451.44 |
|---|---|
| Formula | C22H24F3N3O4 |
| 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 info | Chemical 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 |
| Synonyms | SB-273005; SB 273005; SB273005 |
| 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 Vivo | In 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 model | Thyroidectomized–parathyroidectomized (TPTx) rat model of bone resorption, and ovariectomized (Ovx) rat model of osteoporosis |
| Formulation & Dosage | Dissolved in 1% methylcellulose; 30 mg/kg; i.p. injection |
| References | J Med Chem. 2000 Jan 13;43(1):22-6; Arthritis Rheum. 2001 Jan;44(1):128-37. |
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