cis-ACCP

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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。

CAS NO:

777075-44-2

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
50mg	电议

产品介绍

化学性质

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	222.2
Cas No.	777075-44-2
Formula	C₇H₁₅N₂O₄P
Solubility	≤0.15mg/ml in ethanol;0.3mg/ml in PBS, pH 7.2,
Chemical Name	P-[[[(1R,2S)-2-aminocyclohexyl]amino]carbonyl]-phosphonic acid
Canonical SMILES	N[C@H]1CCCC[C@H]1NC(P(O)(O)=O)=O
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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).