SB273005 INTEGRIN抑制剂
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- CAS号:
- 205678-31-5
- 英文名:
- (S)-2-(8-(2-(6-(methylamino)pyridin-2-yl)ethoxy)-3-oxo-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl)acetic acid
- 英文别名:
- SB273005;[8-[2-(6-Methylamino-pyridin-2-yl)-ethoxy]-3-oxo-2-(2,2,2-trifluoro-ethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl]-acetic acid;1H-2-Benzazepine-4-acetic acid, 2,3,4,5-tetrahydro-8-[2-[6-(methylamino)-2-pyridinyl]ethoxy]-3-oxo-2-(2,2,2-trifluoroethyl)-, (4S)-;(S)-2-(8-(2-(6-(methylamino)pyridin-2-yl)ethoxy)-3-oxo-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl)acetic acid;(S)-2-(8-(2-(6-(methylamino)pyridin-2-yl)ethoxy)-3-oxo-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl)acetic acid USP/EP/BP
- 中文名:
- SB273005 INTEGRIN抑制剂
- 中文别名:
- 化合物SB273005;SB273005 INTEGRIN抑制剂
- CBNumber:
- CB22744623
- 分子式:
- C22H24F3N3O4
- 分子量:
- 451.44
- MOL File:
- 205678-31-5.mol
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SB273005 INTEGRIN抑制剂化学性质
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沸点:
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662.9±55.0 °C(Predicted)
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密度:
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1.321±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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形态:
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Powder
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酸度系数(pKa):
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4.32±0.10(Predicted)
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颜色:
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White to off-white
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SB273005 INTEGRIN抑制剂性质、用途与生产工艺
SB273005 是一种有效的integrin抑制剂,对αvβ3 受体和αvβ5受体的K
i分别为1.2 nM 和 0.3 nM。
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).
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.
SB273005 是一种有效的integrin抑制剂,对αvβ3 受体和αvβ5受体的Ki分别为1.2 nM 和 0.3 nM。
Target | Value |
αvβ5 receptor
(Cell-free assay)
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0.3 nM
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αvβ3 receptor
(Cell-free assay)
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1.2 nM
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在体外,SB273005抑制人破骨细胞介导的骨吸收,IC50 为11 nM。在包含MDA-MB-231细胞的血液中,SB273005与lamifiban结合抑制肿瘤细胞粘附到血管细胞外基质上(ECM)。
在骨吸收和骨质疏松大鼠模型中,SB273005 (30 mg/kg, p.o.)抑制甲状旁腺素刺激的血钙反应,并抑制骨损失。在佐剂性关节炎大鼠体内,SB273005 (60 mg/kg, p.o.)显著减少佐剂诱导的关节炎症状。 在大鼠主动脉和肾动脉中,SB273005 (1000 mg/kg/day, p.o.)引起血管平滑肌细胞(VSMC)急性暂时性坏死。在怀孕的小鼠体内,SB273005逆转Th1细胞产生的IL-2 l水平的下降,以及Th2细胞衍生的IL-10水平的增加。
SB273005 INTEGRIN抑制剂
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/11/08 | S7540 | SB273005 INTEGRIN抑制剂 SB273005 | 205678-31-5 | 5mg | 1595.17元 |
2024/11/08 | S7540 | SB273005 INTEGRIN抑制剂 SB273005 | 205678-31-5 | 10mM(1mL in DMSO) | 2448.81元 |
SB273005 INTEGRIN抑制剂
生产厂家
205678-31-5, SB273005 INTEGRIN抑制剂 相关搜索:
- Inhibitors
- 抑制剂
- 小分子抑制剂,天然产物
- C22H24F3N3O4
- 化合物SB273005
- SB273005 INTEGRIN抑制剂
- 205678-31-5
- (S)-2-(8-(2-(6-(methylamino)pyridin-2-yl)ethoxy)-3-oxo-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl)acetic acid USP/EP/BP
- 1H-2-Benzazepine-4-acetic acid, 2,3,4,5-tetrahydro-8-[2-[6-(methylamino)-2-pyridinyl]ethoxy]-3-oxo-2-(2,2,2-trifluoroethyl)-, (4S)-
- [8-[2-(6-Methylamino-pyridin-2-yl)-ethoxy]-3-oxo-2-(2,2,2-trifluoro-ethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl]-acetic acid
- (S)-2-(8-(2-(6-(methylamino)pyridin-2-yl)ethoxy)-3-oxo-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl)acetic acid
- SB273005