SD-208 blocka TGF-beta-induced phosphorylation of the receptor-associated Smads, Smad2 and Smad3, and stimulates epithelial-to-mesenchymal transdifferentiation, migration, and invasiveness into Matrigel in vitro.In the murine aortic allograft model, SD-208 effectively reduces the formation of intimal hyperplasia of transplant arteriosclerosis (TA).
 |
Source | J Neurosci (2016). Figure 5. SD-208 |
| Method | i.p. | |
| Cell Lines | EAN rats | |
| Concentrations | 20 mg/kg/d | |
| Incubation Time | 12 day | |
| Results | In both the SD-208 alone and RvD1 + SD-208 groups, EAN rats showed much more severe neurological scores and significantly prolonged disease duration, not only compared with the RvD1 + vehicle group, but also compared with the vehicle-alone group (Fig. 5B), suggesting that the inhibition of TGF-β signaling not only abolished the exogenous RvD1 effects, but also may suppress endogenous RvD1 functions. |
| Cell Experiment | |
|---|---|
| Cell lines | Murine SMA-560 or human LN-308 glioma cells |
| Preparation method | Proliferation. Glioma cells were cultured in the absence or presence of SD-208 (1 μmol/L) for 48 hours. The cells were pulsed for the last 24 hours with [methyl-3H]thymidine (0.5 μCi) and harvested (Tomtec, Hamden, CT), and incorporated radioactivity was determined in a liquid scintillation counter (Wallac, Turku, Finland). |
| Concentrations | 1 μM |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | SMA-560 cells bearing VM/Dk mice |
| Formulation | deionized water |
| Dosages | 1 mg/mL |
| Administration | p.o. |
| Molecular Weight | 352.75 |
| Formula | C17H10ClFN6 |
| CAS Number | 627536-09-8 |
| Solubility (25°C) | DMSO 8 mg/mL warmed |
| 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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LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. |
| LSKL, Inhibitor of Thrombospondin (TSP-1)
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