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UK 356618
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
UK 356618图片
CAS NO:230961-08-7
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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。
生物活性

UK 356618 (Compound 4j) is a potent and selective inhibitor ofmatrix metalloprotease-3 (MMP-3)with anIC50of 5.9 nM. UK 356618 is less potent againstMMP-1,MMP-2,MMP-9,MMP-13andMMP-14compared withMMP-3[1].

IC50& Target[1][2]

MMP-3

5.9 nM (IC50)

MMP-13

73 nM (IC50)

MMP-9

0.84 μM (IC50)

MMP-2

1.79 μM (IC50)

MMP-14

1.9 μM (IC50)

MMP-1

51 μM (IC50)

体外研究
(In Vitro)

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[1].
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[2].

体内研究
(In Vivo)

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[3].

Animal Model:Hyperglycemic male Wistar rats injected with middle cerebral artery occlusion (MCAO)[3]
Dosage:15 mg/kg
Administration:Intravenous injection; for 24 h or 7 days
Result:Significantly reduced MMP3 activity in the brain.
分子量

557.72

性状

Solid

Formula

C34H43N3O4

CAS 号

230961-08-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL(44.83 mM;Need ultrasonic and warming)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.7930 mL8.9651 mL17.9301 mL
5 mM0.3586 mL1.7930 mL3.5860 mL
10 mM0.1793 mL0.8965 mL1.7930 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。