Pirfenidone inhibits TGF-β bioactivity by affecting TGF-β2 mRNA expression and processing of pro-TGF-β in CCL-64 cells. In RAW264.7 cells, Pirfenidone suppresses the proinflammatory cytokine TNF-α by a translational mechanism, which is independent of activation of the MAPK2, p38 MAPK, and JNK. In the murine endotoxin shock model, Pirfenidone potently inhibits the production of the proinflammatory cytokines, TNF-α, interferon-γ, and interleukin-6, but enhances the production of the anti-inflammatory cytokine, interleukin-10.
Int J Med Sci. 2020 Jul 2;17(12):1692-1703.
TGFβ1 induces bone formation from BMP9-activated Bone Mesenchymal Stem Cells, with possible involvement of non-canonical pathways
Pirfenidone purchased from AbMole
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Source | Int. J. Med. Sci (2020 Jul). Figure 4. Pirfenidone (Abmole Bioscience, TX, USA) |
| Method | cell culture | |
| Cell Lines | HEK293 and C3H10T1/2 cell lines | |
| Concentrations | 1000 µg/mL | |
| Incubation Time | - | |
| Results | Moreover, pirfenidone could also significantly diminish the protein levels of OPN and OCN |
| Molecular Weight | 185.22 |
| Formula | C12H11NO |
| CAS Number | 53179-13-8 |
| Solubility (25°C) | DMSO 60 mg/mL Water 10 mg/mL (Need ultrasonic) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
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