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227963-15-7

中文名称 化合物 T16085
英文名称 L-000845704
CAS 227963-15-7
分子式 C23H29N5O4
分子量 439.51
MOL 文件 227963-15-7.mol
更新日期 2023/03/20 15:41:25
227963-15-7 结构式 227963-15-7 结构式

基本信息

中文别名
化合物 T16085
英文别名
MK-0429
L-000845704
HGFOOLONGOBCMP-IBGZPJMESA-N
3-Pyridinepropanoic acid, 6-methoxy-β-[2-oxo-3-[3-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)propyl]-1-imidazolidinyl]-, (βS)-

物理化学性质

熔点122 °C
沸点735.5±60.0 °C(Predicted)
密度1.36±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMSO : 250 mg/mL (568.82 mM)
酸度系数(pKa)4.19±0.10(Predicted)
形态Solid
颜色White to off-white

安全数据

危险性符号(GHS)
GHS08
警示词危险
危险性描述H373-H360
防范说明P260-P314-P501

常见问题列表

生物活性
MK-0429 (L-000845704) 是可口服,高效,选择性,非多肽整合素泛拮抗剂,对αvβ1、αvβ3、αvβ5、αvβ6、αvβ8 和 α5β1 的 IC5 0 值分别为1.6 nM、2.8 nM、0.1 nM、0.7 nM、0.5 nM 和 12.2 nM。
靶点

αvβ1

1.6 nM (IC 50 , inhibition of fibronectin-binding )

αvβ3

2.8 nM (IC 50 , inhibition of vitronectin-binding)

αvβ5

0.1 nM (IC 50 , inhibition of vitronectin-binding)

αvβ6

0.7 nM (IC 50 , inhibition of LAP-binding)

αvβ8

0.5 nM (IC 50 , inhibition of LAP-binding)

α5β1

12.2 nM (IC 50 , inhibition of fibronectin-binding)

体内研究

MK-0429 (100 or 300 mg/kg, p.o., twice daily b.i.d., 2 weeks) reduces metastatic tumor colony formation and area in the lungs. MK-0429 is safe and efficacious in significantly decreasing melanoma metastasis in the lungs.

Animal Model: B6D2F1 hybrid female mice
Dosage: 100 or 300 mg/kg
Administration: P.o., twice daily (b.i.d.), 2 weeks
Result: MK-0429 at 100 and 300 mg/kg reduced the number of metastatic tumor colonies by 64 and 57%, respectively, and the high dose also reduced the tumor area by 60% as compared to the vehicle [2] .
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