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PAT-505 is an orally available, selective and potent inhibitor of autologous epidermal growth factor (IC50 2 nM in Hep3B cells, 9.7 nM in human blood, 62 nM in mouse plasma).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $299 | 8-10 weeks |
Description | PAT-505 is an orally available, selective and potent inhibitor of autologous epidermal growth factor (IC50 2 nM in Hep3B cells, 9.7 nM in human blood, 62 nM in mouse plasma). |
Targets&IC50 | Autotaxin (mouse plasma):62 nM, Autotaxin (human blood ):9.7 nM, Autotaxin (Hep3B cells):2 nM |
In vivo | PAT-505 is an effective, selective, and non-competitive inhibitor, exhibiting significant inhibition of ATX activity in plasma and liver tissues upon oral administration. Therapeutic dosing of PAT-505 in Stelic mice model of non-alcoholic steatohepatitis (NASH) resulted in a modest but significant improvement in fibrosis, with only slight improvements in hepatocyte ballooning and liver inflammation. In choline-deficient, high-fat NASH diet model, PAT-505 treatment effectively reduced liver fibrosis, without significant effects on steatosis, hepatocyte ballooning, or inflammation[1]. |
Molecular Weight | 473.92 |
Formula | C23H18ClF2N3O2S |
Cas No. | 1782070-22-7 |
Smiles | CCn1cc(cn1)-n1c(C2CC2)c(Sc2cccc(C(O)=O)c2F)c2ccc(Cl)c(F)c12 |
Relative Density. | 1.53 g/cm3 (Predicted) |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 30 mg/mL (63.30 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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