ARP 101 |
Catalog No.GC12465 |
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 849773-63-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
ARP 101 is a selective MMP-2 inhibitor with IC50 value of 0.81nM.
MMP-2 is an enzyme and 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 [1].
ARP 101 shows inhibition of fibrosarcoma HT1080 cell growth in vitro. ARP 101 has shown ~250 fold selectivity of MMP-2 over MMP-1 and ~100 fold of MMP-9 over MMP-1 [2]. ARP 101 proved to be 15.3 and 24.7 times more potent than compound a and CGS 27023A on MMP-2, maintaining a different selectivity and potency of MMP-2/MMP-1 compared with inhibitor Prinomastat and CGS 27023A [3].
Reference:
[1]. Page-McCaw A, Ewald AJ, Werb Z. Matrix metalloproteinases and the regulation of tissue remodelling. Nat Rev Mol Cell Biol, 2007, 8(3): 221-33.
[2]. Rossello A, Nuti E, Orlandini E, et al. New N-arylsulfonyl-N-alkoxyaminoacetohydroxamic acids as selective inhibitors of gelatinase A (MMP-2). Bioorg Med Chem, 2004, 12(9): 2441-50.
[3]. Tuccinardi T, Martinelli A, Nuti E, et al. 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, 2004, 14: 4260-4276.
Cas No. | 849773-63-3 | SDF | |
Chemical Name | (R)-N-hydroxy-2-(N-isopropoxy-[1,1'-biphenyl]-4-ylsulfonamido)-3-methylbutanamide | ||
Canonical SMILES | CC(C)[C@@H](N(OC(C)C)S(=O)(C1=CC=C(C2=CC=CC=C2)C=C1)=O)C(NO)=O | ||
Formula | C20H26N2O5S | M.Wt | 406.5 |
Solubility | <40.65mg/ml in DMSO; <10.16mg/ml in ethanol | Storage | Desiccate at 4°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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.46 mL | 12.3001 mL | 24.6002 mL |
5 mM | 0.492 mL | 2.46 mL | 4.92 mL |
10 mM | 0.246 mL | 1.23 mL | 2.46 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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.)
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.
Average Rating: 5
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