| Identification | Back Directory | [Name]
CTS-1027 | [CAS]
193022-04-7 | [Synonyms]
CTS-1027
RS130830
RS-130830
RS 130830
Ro1130830
Ro-1130830
Ro 1130830
RS 130830, Ro-1130830
RS 130830;RO 1130830;CTS1027;CTS 1027;RS130830;RO1130830;RS-130830;RO-1130830
4-[[[4-(4-Chlorophenoxy)phenyl]sulfonyl]methyl]tetrahydro-N-hydroxy-2H-pyran-4-carboxamide
2H-Pyran-4-carboxaMide, 4-[[[4-(4-chlorophenoxy)phenyl]sulfonyl]Methyl]tetrahydro-N-hydroxy- | [Molecular Formula]
C19H20ClNO6S | [MDL Number]
MFCD16657131 | [MOL File]
193022-04-7.mol | [Molecular Weight]
425.88 |
| Chemical Properties | Back Directory | [density ]
1.388±0.06 g/cm3(Predicted) | [storage temp. ]
Inert atmosphere,Store in freezer, under -20°C | [solubility ]
Soluble in DMSO | [form ]
A solid | [pka]
9.27±0.23(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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. | [Biological Activity]
CTS-1027 is a potent MMP inhibitor with IC50 values of 0.3 nM and 0.5 nM for MMP2 and MMP13, respectively. | [in vivo]
CTS-1027 significantly reduces the hepatocyte apoptosis, features of cholestatic liver injury, amd markers of hepatic fibrogenesis in the BDL mouse. It improves overall animal survival following 14 days of BDL in mice. 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 Plaque. The lipid content of animals receiving RS-130830 is increased by 81% at 12 weeks, and increased by 41% at 16 weeks. div> | [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) | [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. DOI:10.1111/j.1872-034X.2009.00541.x
[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. DOI:10.1016/j.cardiores.2006.05.009 |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
|
| Website: |
www.spiropharma.com.cn |
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