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cis-ACCP
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。
cis-ACCP图片
CAS NO:777075-44-2
规格:98%
分子量:222.2
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议

产品介绍
type IV collagen-specific MMP-2 and MMP-9 inhibitor
CAS:777075-44-2
分子式:C7H15N2O4P
分子量:222.2
纯度:98%
存储:Store at -20°C

Background:

IC50: 4 and 20 μM for MMP-2 and MMP-9, respectively


cis-ACCP is a type IV collagen-specific MMP-2 and MMP-9 inhibitor.


Matrix metalloproteinases (MMPs) belong to a family of proteases that play a keyrole in tissue remodeling and repair via degrading extracellular matrix proteins, therefore enabling cell migration.


In vitro: cis-ACCP could preferentially inhibit MMP-2 and MMP-9 with a preference for MMP-2. The trans-ACCP did not inhibit the gelatinases but had moderate activity against MMP-3 and MMP-13. These findings indicated specificity of the compounds regarding binding to the enzymes. Furthermore, addition of cis-ACCP to tumor cells was able to prevent their traversion dose-dependently, about 90% at the highest concentration tested [1].


In vivo: Aninmal study showd that cis-ACCP could reduce metastasis formation in mice by approximately 90% when administered by a repetitive once daily dosing regimen at 50 mg/kg via oral or i.p. routes and was nontoxic up to 500 mg/kg, following i.p. administration daily for two weeks. In addition, the pharmacokinetic investigation in rats revealed distribution restricted into the extracellular fluid, the site of action for the antimetastatic activity and rapid elimination from blood [1].


Clinical trial: So far, no clinical study has been conducted.


Reference:
[1] Hoffman, A. ,Qadri, B.,Frant, J., et al. Carbamoylphosphonate matrix metalloproteinase inhibitors 6: Cis-2-aminocyclohexylcarbamoylphosphonic acid, a novel orally active antimetastatic matrix metalloproteinase-2 selective inhibitor-synthesis and pharmacodynamic and pharmacokinetic analysis. Journal of Medicinal Chemistry 51, 1406-1414 (2008).