Home>>Signaling Pathways>> Proteases>> Elastase>>ARP 100

ARP 100 (Synonyms: CAY10609, Matrix Metalloproteinase-2 Inhibitor III, MMP2 Inhibitor III)

Catalog No.GC13487

A selective inhibitor of MMP-2

Products are for research use only. Not for human use. We do not sell to patients.

ARP 100 Chemical Structure

Cas No.: 704888-90-4

Size Price Stock Qty
1mg
$17.00
In stock
5mg
$72.00
In stock
10mg
$117.00
In stock

Tel:(909) 407-4943 Email: sales@glpbio.com

Customer Reviews

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Background

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.

Chemical Properties

Cas No. 704888-90-4 SDF
Synonyms CAY10609, Matrix Metalloproteinase-2 Inhibitor III, MMP2 Inhibitor III
Chemical Name N-hydroxy-2-[(4-phenylphenyl)sulfonyl-propan-2-yloxyamino]acetamide
Canonical SMILES CC(C)ON(CC(=O)NO)S(=O)(=O)C1=CC=C(C=C1)C2=CC=CC=C2
Formula C17H20N2O5S M.Wt 364.42
Solubility 25mg/mL in DMSO, 25mg/mL in DMF, 30mg/mL in Ethanol Storage Desiccate at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.7441 mL 13.7204 mL 27.4409 mL
5 mM 0.5488 mL 2.7441 mL 5.4882 mL
10 mM 0.2744 mL 1.372 mL 2.7441 mL
  • Molarity Calculator

  • Dilution Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

Review for ARP 100

Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for ARP 100

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.