1. Metabolic Enzyme/Protease
  2. MMP
  3. CTS-1027

CTS-1027 (Synonyms: Ro 1130830; RS 130830)

Cat. No.: HY-10398 Purity: 98.45%
Handling Instructions

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.

For research use only. We do not sell to patients.

CTS-1027 Chemical Structure

CTS-1027 Chemical Structure

CAS No. : 193022-04-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 232 In-stock
Estimated Time of Arrival: December 31
5 mg USD 211 In-stock
Estimated Time of Arrival: December 31
10 mg USD 396 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1162 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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.

IC50 & Target

IC50: 0.2 nM (MMP2), 0.5 nM (MMP13), 0.7 nM (MMP12), 0.9 nM (MMP8), 9.5 nM (MMP3), 15 nM (MMP14)

In Vivo

CTS-1027 significantly reduces the hepatocyte apoptosis, features of cholestatic liver injury, amd markers of hepatic fibrogenesis in the BDL mouse. CTS-1027 improves overall animal survival following 14 days of BDL in mice[1]. In male animals treated for 8 weeks the terminal plasma concentration of RS-130830 is 311±45 nM. Treatment of male mice with RS-130830 for 8 weeks causes an 89% increase in plasma triglyceride concentration, but there is no corresponding effect in female mice treated for 12 weeks. The plaque lipid content of animals receiving RS-130830 is increased by 81% at 12 weeks, and increased by 41% at 16 weeks[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

425.88

Formula

C₁₉H₂₀ClNO₆S

CAS No.

193022-04-7

SMILES

O=C(NO)C1(CCOCC1)CS(=O)(C2=CC=C(C=C2)OC3=CC=C(C=C3)Cl)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (234.81 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3481 mL 11.7404 mL 23.4808 mL
5 mM 0.4696 mL 2.3481 mL 4.6962 mL
10 mM 0.2348 mL 1.1740 mL 2.3481 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.87 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

CTS-1027Ro 1130830 RS 130830CTS1027CTS 1027Ro1130830Ro-1130830RS130830RS 130830RS-130830MMPMatrix metalloproteinasesInhibitorinhibitorinhibit

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