產(chǎn)品目錄

規(guī)格	5mg 10mg 1mg
CAS	704888-90-4
別名	CAY10609
化學(xué)名	N-hydroxy-2-[(4-phenylphenyl)sulfonyl-propan-2-yloxyamino]acetamide
分子式	C17H20N2O5S
分子量	364.42
溶解度	25mg/mL in DMSO, 25mg/mL in DMF, 30mg/mL in Ethanol
儲(chǔ)存條件	Desiccate 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：

ARP 100 is a selective inhibitor of matrix metalloproteinases 2 (MMP-2) with IC50 value of 12 nM [1].

Proteins of the matrix metalloproteinase (MMP) family are involved in the breakdown of extracellular matrix in normal physiological processes, such as embryonic development, reproduction, and tissue remodeling, as well as in disease processes, such as arthritis and metastasis (http://en.wikipedia.org/wiki/MMP2). ARP 100 is a selective inhibitor of matrix metalloproteinases 2 (MMP-2).

In vitro: As a potent derivative of N-arylsulfonyl-N-alkoxyaminoacetohydroxamic acids, ARP 100, shows similar anti-invasive properties to the analogue reference drug CGS27023A, in an in vitro model of invasion on matrigel, carried out on cellular lines of fibrosarcoma HT1080 (tumoural cells over-expressing MMP-2 and MMP-9) [1].

In silico: ARP 100 proved to be practically inactive in the MMP-1; this was probably due to the presence of the biphenyl group, since this substituent was not able to interact in the S10 pocket, and this fact determined the loss of the interaction of the oxygen atoms of the sulfonamido group with Ala182 and Leu181. ARP 100 was also found to be the most selective ligand of the four analyzed, and this fact could be due to the presence of a large P10 group, rigid and unable to form H bonds, or to interact with the MMP-1-S10 pocket. This analysis suggested that in order to maintain the MMP-2/MMP-1 selectivity, the presence of the biphenyl group as a P10 substituent could be very useful [2].

Clinical trial: ARP 100 is currently in the preclinical development and no clinical trial is ongoing.

References:

[1] Rossello A, Nuti E, Orlandini E, Carelli P, Rapposelli S, Macchia M, Minutolo F, Carbonaro L, Albini A, Benelli R, Cercignani G, Murphy G, Balsamo A. New N-arylsulfonyl-N- alkoxyaminoacetohydroxamic acids as selective inhibitors of gelatinase A (MMP-2). Bioorg Med Chem. 2004;12(9):2441-50.

[2] Tuccinardi T, Martinelli A, Nuti E, Carelli P, Balzano F, Uccello-Barretta G, Murphy G, Rossello A.Amber force field implementation, molecular modelling study, synthesis and MMP-1/MMP-2 inhibition profile of (R)- and (S)-N-hydroxy-2-(N-isopropoxybiphenyl-4-ylsulfonamido)- 3-methylbutanamides. Bioorg Med Chem. 2006;14(12):4260-76.

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1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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