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530141-72-1

530141-72-1 structure
530141-72-1 structure
  • Name: T-5224
  • Chemical Name: 3-[5-[4-(cyclopentoxy)-2-hydroxy-benzoyl]-2-[(3-hydroxy-1,2-benzo xazol-6-yl)methoxy]phenyl]propanoic acid
  • CAS Number: 530141-72-1
  • Molecular Formula: C29H27NO8
  • Molecular Weight: 517.527
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease MMP
  • Create Date: 2017-04-17 05:10:07
  • Modify Date: 2024-01-02 01:36:45
  • T-5224 is a selective inhibitor of c-Fos/activator protein (AP)-1. It also inhibits MMP3/13 with IC50s of 10 nM.
Name 3-[5-[4-(cyclopentoxy)-2-hydroxy-benzoyl]-2-[(3-hydroxy-1,2-benzo xazol-6-yl)methoxy]phenyl]propanoic acid
Synonyms 3-{5-[4-(Cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-oxo-2,3-dihydro-1,2-benzoxazol-6-yl)methoxy]phenyl}propanoic acid
Benzenepropanoic acid, 5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(2,3-dihydro-3-oxo-1,2-benzisoxazol-6-yl)methoxy]-
T-5224
Description T-5224 is a selective inhibitor of c-Fos/activator protein (AP)-1. It also inhibits MMP3/13 with IC50s of 10 nM.
Related Catalog
Target

IC50: 10 nM (MMP-3), 10 nM (MMP-13)

In Vitro T-5224 (0-80 μM) significantly inhibits the invasion, migration, and MMP activity of HSC-3-M3 cells in a dose-dependent manner. There is no significant influence on HSC-3-M3 amd OSC-19 cells proliferation[4].
In Vivo G2 is observed in rat and monkey liver microsomes as a major metabolite of T-5224, suggesting that G2 is not a human-specific metabolite[1]. T-5224 (300 mg/kg, p.o.) inhibits the production of TNF-alpha and other downstream effectors in C57BL/6 mice[2]. Administration of T-5224 (300 mg/kg, p.o.) after intraperitoneal injection of LPS impartes appreciable protection against acute elevations in serum levels of TNFα, HMGB1, ALT/AST as well as in liver tissue levels of MIP-1α and MCP-1, and reduces the lethality (27%)[3].
Cell Assay HSC-3-M3 cells are starved for 24 h with DMEM containing 0.5% FBS. The top chamber of the cell invasion device is coated with 50 μL of 0.1 × basement membrane extract solution and incubataed overnight. HSC-3-M3 cells (5.0 × 104 cells/well) are added to the top chamber with DMEM containing 0.5% FBS mixed with 0-80 μM T-5224; DMEM with 10% FBS is added to the bottom chamber and incubated for 48 h. The bottom plate is read using a multilabel plate reader. The data are compared with the standard curve to determine the fraction of invaded cells.
Animal Admin Mice in LPS group are administered orally with polyvinylpyrrolidone solution in the same volume of T-5224 solution immediately after LPS injection, while in the T-5224 group, mice are administered orally with T-5224 (300 mg/kg, p.o.) in the same manner. In the control group, mice receives polyvinylpyrrolidone solution orally soon after intraperitoneal saline injection. Blood samples are collected for each measurement at the optimal time.
References

[1]. Uchihashi S, et al. Metabolism of the c-Fos/activator protein-1 inhibitor T-5224 by multiple human UDP-glucuronosyltransferase isoforms. Drug Metab Dispos. 2011 May;39(5):803-13.

[2]. Miyazaki H, et al. The effects of a selective inhibitor of c-Fos/activator protein-1 on endotoxin-induced acute kidney injury in mice. BMC Nephrol. 2012 Nov 23;13:153.

[3]. Izuta S, et al. T-5224, a selective inhibitor of c-Fos/activator protein-1, attenuates lipopolysaccharide-induced liver injury in mice. Biotechnol Lett. 2012 Dec;34(12):2175-82.

[4]. Kamide D, et al. Selective activator protein-1 inhibitor T-5224 prevents lymph node metastasis in an oral cancer model. Cancer Sci.?2016 May;107(5):666-73.

[5]. Zeng H, et al. An Isogenic Human ESC Platform for Functional Evaluation of Genome-wide-Association-Study-Identified Diabetes Genes and Drug Discovery. Cell Stem Cell. 2016 Sep 1;19(3):326-40.

[6]. Mukherjee A, et al. Infralimbic cortex is required for learning alternatives to prelimbic promoted associations through reciprocal connectivity. Nat Commun. 2018 Jul 13;9(1):2727.
Density 1.4±0.1 g/cm3
Boiling Point 774.1±60.0 °C at 760 mmHg
Molecular Formula C29H27NO8
Molecular Weight 517.527
Flash Point 422.0±32.9 °C
Exact Mass 517.173645
PSA 139.32000
LogP 5.14
Vapour Pressure 0.0±2.8 mmHg at 25°C
Index of Refraction 1.665
Storage condition 2-8°C
Hazard Codes Xi

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title: CAS No. 530141-72-1 | Chemsrc address: https://m.chemsrc.com/en/baike/688205.html

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