CTS-1027

MMPs inhibitor CAS# 193022-04-7

CTS-1027

Catalog No. BCC1502----Order now to get a substantial discount!

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Chemical structure

CTS-1027

3D structure

Chemical Properties of CTS-1027

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.
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.
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.

Biological Activity of CTS-1027

DescriptionCTS-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.
TargetsMMP-2MMP-13MMP-1   
IC500.4 nM0.6 nM800 nM    

Protocol

Animal Administration [1]
For experimental procedures, mice are anesthetized with ketamine 60 mg/kg plus xylazine 10 mg/kg body weight by intraperitoneal injection. After a midline upper-abdominal incision, the peritoneal cavity is opened, the abdominal wall retracted, and the common hepatic bile duct is double-ligated below the bifurcation and transected between the ligatures as previously described by us in detail. Sham-operated mice, used as controls, also underwent similar laparotomy with exposure but without ligation of the common bile duct. The fascia and skin of the midline abdominal incision are closed with sterile surgical 5-0 sutures. Either CTS-1027 or the vector carboxymethylcellulose are administered by gavage in a dose of 10 mg/kg body weight once a day. Drugs are prepared freshly on the day of the study. After 14 days of BDL and gavage, mice are re-anesthetized, sacrificed and blood is obtained from the inferior vena cava for serum total bilirubin and ALT determinations and the liver is removed, cut into small pieces and either snap-frozen in liquid nitrogen for storage at −80°C or fixed in freshly prepared 4% paraformaldehyde in phosphate-buffered saline (PBS) for 48 hours at 4°C for additional studies. Liver tissue is also subjected to RNA extraction using the Trizol reagent. Serum bilirubin and ALT determinations are performed as previously described.

References:
[1]. Kahraman A, et al. Matrix metalloproteinase inhibitor, CTS-1027, attenuates liver injury and fibrosis in the bile duct-ligated mouse. Hepatol Res. 2009 Aug;39(8):805-813. [2]. Johnson JL, et al. Effect of broad-spectrum matrix metalloproteinase inhibition on atherosclerotic plaque stability. Cardiovasc Res. 2006 Aug 1;71(3):586-595.

CTS-1027 Dilution Calculator

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CTS-1027 Molarity Calculator

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Preparing Stock Solutions of CTS-1027

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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Background on CTS-1027

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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References on CTS-1027

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.

Description

CTS-1027 is a potent small molecule inhibitor of MMPs, with IC50s of 0.3 nM, 0.5 nM for MMP2, MMP13, respectively, and has > 1,000 fold selectivity over MMP1.

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