產(chǎn)品屬性:
產(chǎn)品名稱 | 規(guī)格 | CAS號 | 型號 |
cis-ACCP | 1mg 5mg 10mg 50mg | 777075-44-2 | EY-Y0164070 |
Cas No.777075-44-2
別名
化學(xué)名 P-[[[(1R,2S)-2-aminocyclohexyl]amino]carbonyl]-phosphonic acid
分子式 C7H15N2O4P
分子量 222.2
溶解度 ≤0.15mg/ml in ethanol;0.3mg/ml in PBS, pH 7.2,
儲存條件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述:
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).
關(guān)鍵字: 777075-44-2;C7H15N2O4P;cis-ACCP;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學(xué)、分子生物學(xué)和常規(guī)生化試劑等為一體的科研產(chǎn)品銷售企業(yè),公司自成立以來,秉承""全心全意服務(wù)于科研工作者""的企業(yè)理念,立足生物科技領(lǐng)域,運用生物技術(shù)和科研試劑,發(fā)展現(xiàn)代生物科技,為各類大中小醫(yī)院及其它醫(yī)療機構(gòu)、高等院校、科研院所、企事業(yè)單位提供優(yōu)質(zhì)的產(chǎn)品,服務(wù)生物科技領(lǐng)域的科學(xué)研究人員。
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