UK 356618

生物活性靶点体外研究体内研究 UK 356618 试剂级价格

UK 356618

CAS号:230961-08-7
英文名:N1-[(1S)-2,2-Dimethyl-1-[[[(1R)-1-phenylethyl]amino]carbonyl]propyl]-N4-hydroxy-2-[3-(2-methyl[1,1'-biphenyl]-4-yl)propyl]-butanediamine
中文名:UK 356618
CBNumber:CB82518853
分子式:C34H43N3O4
分子量:557.72
MOL File:230961-08-7.mol

UK 356618化学性质

熔点 :93-102oC
密度 :1.124±0.06 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO: ≥25mg/mL
形态 :powder
酸度系数(pKa) :9.16±0.20(Predicted)
颜色 :white to tan
旋光性 (optical activity) :[α]/D >+25.0°, c = 0.5 in methanol

安全信息

危险品标志 :Xn
危险类别码 :22
WGK Germany :3

UK 356618性质、用途与生产工艺

生物活性 UK 356618 (Compound 4j) 是一种有效且选择性的基质金属蛋白酶 3 (MMP-3) 抑制剂，其 IC50 值为 5.9 nM。与 MMP-3相比，UK 356618 对 MMP-1，MMP-2，MMP-9， MMP-13 和 MMP-14 的抑制效力较低。

靶点

MMP-3

5.9 nM (IC ₅₀ )

MMP-13

73 nM (IC ₅₀ )

MMP-9

0.84 μM (IC ₅₀ )

MMP-2

1.79 μM (IC ₅₀ )

MMP-14

1.9 μM (IC ₅₀ )

MMP-1

51 μM (IC ₅₀ )

体外研究

Inhibition of MMP-3 and selectivity over MMP-2 was remarkably sensitive to the size of the substituent and is clearly optimal for a methyl group (UK 356618, compound 4j). UK 356618 is more widely profiled against other MMPs.
MMP-13 is closely involved in IL-6 or TNF-α increasing tumor metastasis. MMP-13 deficiency abrogate TNF-α effect on lung cancer cell migration. UK 356618 treatment efficiently abolished the effect of TNF-α on cell migration in NCI-H446 cells.

体内研究

UK 356618 (15 mg/kg; intravenous injection; for 24 h or 7 days; male Wistar rats) treatment at reperfusion significantly reduces MMP3 activity in the brain.

Animal Model:	Hyperglycemic male Wistar rats injected with middle cerebral artery occlusion (MCAO)
Dosage:	15 mg/kg
Administration:	Intravenous injection; for 24 h or 7 days
Result:	Significantly reduced MMP3 activity in the brain.