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T-5224

Cat. No. M9373
T-5224 Structure
Size Price Availability Quantity
10mM*1mL in DMSO USD 122  USD122 In stock
2mg USD 70  USD70 In stock
5mg USD 110  USD110 In stock
10mg USD 165  USD165 In stock
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Quality Control & Documentation
Biological Activity

T-5224 inhibits the IL-1β-induced up-regulation of Mmp-3, Mmp-13 and Adamts-5 transcription. T-5224 (0-80 μM) significantly inhibits the invasion, migration, and MMP activity of HSC-3-M3 cells in a dose-dependent manner.

In vivo, 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%). T-5224 (300 mg/kg, p.o.) inhibits the production of TNF-alpha and other downstream effectors in C57BL/6 mice.

Product Citations
Chemical Information
Molecular Weight 517.53
Formula C29H27NO8
CAS Number 530141-72-1
Solubility (25°C) DMSO ≥ 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Makino H, et al. Sci Rep. A selective inhibition of c-Fos/activator protein-1 as a potential therapeutic target for intervertebral disc degeneration and associated pain.

[2] Kamide D, et al. Cancer Sci. Selective activator protein-1 inhibitor T-5224 prevents lymph node metastasis in an oral cancer model.

[3] Miyazaki H, et al. BMC Nephrol. The effects of a selective inhibitor of c-Fos/activator protein-1 on endotoxin-induced acute kidney injury in mice.

[4] Shinichiro Izuta, et al. Biotechnol Lett . T-5224, a selective inhibitor of c-Fos/activator protein-1, attenuates lipopolysaccharide-induced liver injury in mice

[5] Yukihiko Aikawa, et al. Nat Biotechnol . Treatment of arthritis with a selective inhibitor of c-Fos/activator protein-1

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