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
- 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
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。
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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 )
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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.
- 更新日期：2024/04/30
- 产品编号：HY-107394
- 产品名称：UK 356618 UK 356618
- CAS编号：230961-08-7
- 包装：1mg
- 价格：1700元
- 更新日期：2024/04/30
- 产品编号：HY-107394
- 产品名称：UK 356618
- CAS编号：
- 包装：10 mM * 1 mLin DMSO
- 价格：5610元
- 公司名称：Carbosynth
- 联系电话：--
- 电子邮件：sales@carbosynth.com
- 国家：英国
- 产品数：6018
- 优势度：58
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5729
- 优势度：77
