CTS-1027MMPs inhibitor CAS# 193022-04-7 |
Quality Control & MSDS
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| Cas No. | 193022-04-7 | SDF | Download SDF |
| PubChem ID | 3342298 | Appearance | Powder |
| Formula | C19H20ClNO6S | M.Wt | 425.88 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Ro 1130830; RS 130830 | ||
| Solubility | DMSO : ≥ 100 mg/mL (234.81 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 4-[[4-(4-chlorophenoxy)phenyl]sulfonylmethyl]-N-hydroxyoxane-4-carboxamide | ||
| SMILES | C1COCCC1(CS(=O)(=O)C2=CC=C(C=C2)OC3=CC=C(C=C3)Cl)C(=O)NO | ||
| Standard InChIKey | ROSNVSQTEGHUKU-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C19H20ClNO6S/c20-14-1-3-15(4-2-14)27-16-5-7-17(8-6-16)28(24,25)13-19(18(22)21-23)9-11-26-12-10-19/h1-8,23H,9-13H2,(H,21,22) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | CTS-1027 is an orally bioavailable and small-molecule inhibitor of matrix metalloproteinases (MMPs) with IC50 values of 0.4 nM, 0.6 nM and 800 nM for MMP-2, MMP-13 and MMP-1, respectively. | |||||
| Targets | MMP-2 | MMP-13 | MMP-1 | |||
| IC50 | 0.4 nM | 0.6 nM | 800 nM | |||
CTS-1027 Dilution Calculator
CTS-1027 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.3481 mL | 11.7404 mL | 23.4808 mL | 46.9616 mL | 58.702 mL |
| 5 mM | 0.4696 mL | 2.3481 mL | 4.6962 mL | 9.3923 mL | 11.7404 mL |
| 10 mM | 0.2348 mL | 1.174 mL | 2.3481 mL | 4.6962 mL | 5.8702 mL |
| 50 mM | 0.047 mL | 0.2348 mL | 0.4696 mL | 0.9392 mL | 1.174 mL |
| 100 mM | 0.0235 mL | 0.1174 mL | 0.2348 mL | 0.4696 mL | 0.587 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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CTS-1027 is a selective inhibitor of MMP with IC50 value of 0.4 nM for MMP 2 and 0.6 nM for MMP13 [1].
MMPs (matrix metalloproteinase) are zinc-dependent endopeptidases and play an important role in degrading all kinds of extracellular matrix proteins. It is well known that MMPs involve in the cleavage of cell surface receptors, the release of apoptotic ligands, and inactivation chemokine/cytokine. And MMPs also play a pivotal role in cell proliferation, migration, differentiation, angiogenesis, apoptosis and host defense [2] [3].
In C57/BL6 mice model suffered bile duct ligation (BDL) for 14 days, gavage CTS-1027 reduced apoptosis of hepatocyte and bile infarcts which was a histologic indicator of liver injury at the same time activated stellate cells and reduced hepatic fibrogenesis [4].
References:
[1]. Barta, T.E., et al., Selective, orally active MMP inhibitors with an aryl backbone. Bioorg Med Chem Lett, 2001. 11(18): p. 2481-3.
[2]. Toth, M., A. Sohail, and R. Fridman, Assessment of gelatinases (MMP-2 and MMP-9) by gelatin zymography. Methods Mol Biol, 2012. 878: p. 121-35.
[3]. Roomi, M.W., et al., Patterns of MMP-2 and MMP-9 expression in human cancer cell lines. Oncol Rep, 2009. 21(5): p. 1323-33.
[4]. Kahraman, A., et al., Matrix metalloproteinase inhibitor, CTS-1027, attenuates liver injury and fibrosis in the bile duct-ligated mouse. Hepatol Res, 2009. 39(8): p. 805-13.
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Matrix metalloproteinase inhibitor, CTS-1027, attenuates liver injury and fibrosis in the bile duct-ligated mouse.[Pubmed:19624765]
Hepatol Res. 2009 Aug;39(8):805-13.
AIM: Excessive matrix metalloproteinase (MMP) activity has been implicated in the pathogenesis of acute and chronic liver injury. CTS-1027 is an MMP inhibitor, which has previously been studied in humans as an anti-arthritic agent. Thus, our aim was to assess if CTS-1027 is hepato-protective and anti-fibrogenic during cholestatic liver injury. METHODS: C57/BL6 mice were subjected to bile duct ligation (BDL) for 14 days. Either CTS-1027 or vehicle was administered by gavage. RESULTS: BDL mice treated with CTS-1027 demonstrated a threefold reduction in hepatocyte apoptosis as assessed by the TUNEL assay or immunohistochemistry for caspase 3/7-positive cells as compared to vehicle-treated BDL animals (P < 0.01). A 70% reduction in bile infarcts, a histological indicator of liver injury, was also observed in CTS-1027-treated BDL animals. These differences could not be ascribed to differences in cholestasis as serum total bilirubin concentrations were nearly identical in the BDL groups of animals. Markers for stellate cell activation (alpha-smooth muscle actin) and hepatic fibrogenesis (collagen 1) were reduced in CTS-1027 versus vehicle-treated BDL animals (P < 0.05). Overall animal survival following 14 days of BDL was also improved in the group receiving the active drug (P < 0.05). CONCLUSION: The BDL mouse, liver injury and hepatic fibrosis are attenuated by treatment with the MMP inhibitor CTS-1027. This drug warrants further evaluation as an anti-fibrogenic drug in hepatic injury.
