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192329-42-3

中文名称 普马司他
英文名称 Prinomastat
CAS 192329-42-3
分子式 C18H21N3O5S2
分子量 423.51
MOL 文件 192329-42-3.mol
更新日期 2023/03/20 15:41:26
192329-42-3 结构式 192329-42-3 结构式

基本信息

中文别名
普马司他
普啉司他
MMP抑制剂(PRINOMASTAT)
(S)-2-[(羟基氨基)甲基]-5,6-二甲基-4-(4-吡啶-4-基氧苯基)磺酰基吗啉-3-硫酮
英文别名
Ag3340
Ag 3340
Ag-3340
KB-R 9896
Prinomastat
AG3340 hydrochloride
AG 3340 hydrochloride
AG-3340 hydrochloride
Prinomastat hydrochloride
(S)-2,2-DIMETHYL-N-HYDROXY-4-[4-(4-PYRIDYLOXY)PHENYLSULFONYL]-1,4-THIAZINANE-3-CARBOXAMIDE

物理化学性质

熔点149.8°
储存条件room temp
溶解度在水中的溶解度为15mg/mL(澄清溶液)
形态粉末
颜色白色至米色

安全数据

危险性符号(GHS)
GHS08
警示词危险
危险性描述H360
防范说明P201-P308+P313
危险品标志T
危险类别码60-61
安全说明53-45
WGK Germany3
普马司他价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/08/19HY-12170A普马司他
Prinomastat hydrochloride
192329-42-31mg1250元
2024/08/19HY-12170A普马司他
Prinomastat hydrochloride
192329-42-35mg3750元
2024/08/19HY-12170A普马司他
Prinomastat hydrochloride
192329-42-310mM * 1mLin DMSO3795元

常见问题列表

生物活性
Prinomastat (AG3340) 是一种广谱,有效的口服活性金属蛋白酶 (MMP) 抑制剂,对于 MMP-1, MMP-3 和 MMP-9 的 IC50 分别为 79 nM,6.3 nM 和 5.0 nM。Prinomastat 抑制 MMP-2, MMP-3 和 MMP-9 的 Ki 分别为 0.05 nM,0.3 nM 和 0.26 nM。Prinomastat 穿过血脑屏障。抗肿瘤活性。
靶点

MMP-9

5 nM (IC 50 )

MMP-9

0.26 nM (Ki)

MMP-2

0.05 nM (Ki)

MMP-1

79 nM (IC 50 )

MMP-3

6..3 nM (IC 50 )

MMP-3

0.3 nM (Ki)

体外研究

Prinomastat (AG3340; 0.1-1 µg/mL; 4 days; C57MG/Wnt1 cells) inhibits Wnt1-induced MMP-3 production. Reversal of Wnt1-induced EMT and β-catenin transcriptional activity by Prinomastat.
Co-culture of L/Wnt3a cells and CT7 cells increases the Topflash activity in CT7 cells, and co-culturing both L/Wnt3a cells and MMP-3 overexpressing C57MG cells with CT7 cells increases the Topflash luciferase activity in CT7 cells beyond the level observed with L/Wnt3a cells, and these effects are all suppressed by Prinomastat (AG3340).
Inhibition of entry of C57MG/Wnt1 cells into S phase by Prinomastat corresponds to a decrease in expression of cyclin D1 and Erk1/2 phosphorylation. The effect of Prinomastat on Wnt1-induced migration is then examined using an in vitro wound assay. As anticipated, the migration of C57MG/Wnt1 cells is increased by 1.8-fold when compared with C57MG cells.The effect of Wnt1 on the cellular distribution of vimentin is reversed by Prinomastat in C57MG/Wnt1 cells.

Western Blot Analysis

Cell Line: C57MG/Wnt1 cells
Concentration: 0.1 µg/mL, 1 µg/mL
Incubation Time: 4 days
Result: A significant decrease in MMP-3 promoter activity in C57MG/Wnt1 cells.
体内研究

In a human fibrosarcoma mouse model (HT1080), the mice are treated therapeutically for 14-16 days with 50 mg/kg/day ip daily starting day 3 to 6 after tumour inoculation. Prinomastat is well tolerated by the animals, and there are no signs of weight loss or other adverse effects. Prinomastat has good tumour growth inhibition, with a short T 1/2 of 1.6 hours.

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