Suplatast tosylate is a Th2 cytokine inhibitor which is used as an anti-allergic drug. Suplatast tosylate is a novel anti-allergic agent that suppresses several processes, including the synthesis of IL-4 and IL-5 in both human and murine Th2 (-like) cells; IgE synthesis in both mice and humans, with no direct effect on B cells; local eosinophilia regulated by Th2 cells in mice; and infiltration of both eosinophils and CD41 T cells into the airways, with consequent airway hyperresponsiveness after allergen inhalation in sensitized guinea pigs.
| Cell Experiment | |
|---|---|
| Cell lines | Dendritic cells (DCs) and CD4+ T cells |
| Preparation method | Using magnetic cell separation system micro-beads and columns, allogeneic responder CD4+ T cells which are obtained from healthy subjects are purified from PBMCs by negative depletion of CD14+, CD16+, CD19+, CD56+, and CD8+ cells . After 7 days of culture with GM-CSF and IL-4, iDCs which are differentiated from monocytes in the presence or absence of Suplatast tosilate (10 and 100 mg/ mL), are co-cultured with purified 1×10 5 allogeneic CD41 T cells at varying ratios of iDCs in 96-well round bottomed culture plates for 5 days. Pulsing cells with 1 μCi of 3H-methylthymidine for the last 8 hours of the culture period. Counting incorporated radioactivity with a liquid scintillation counter, and expressing proliferative responses as the mean 3 H-methylthymidine incorporation (counts per minutes) of triplicate wells_SEM. Also, assessing proliferation of DCs alone or CD4+ T cells alone. |
| Concentrations | 10 or 100 μg/mL |
| Incubation time | 5 days |
| Animal Experiment | |
|---|---|
| Animal models | BALB/c mice sensitized to ovalbumin |
| Formulation | Dissolved in sterile saline. |
| Dosages | 100 mg/kg/100 μL |
| Administration | Orally once a day for 21 days |
| Molecular Weight | 499.64 |
| Formula | C23H33NO7S2 |
| CAS Number | 94055-76-2 |
| Solubility (25°C) | DMSO 90 mg/mL |
| 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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