Home Immunology & Inflammation Interleukins antagonist Suplatast Tosylate

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Suplatast Tosylate Interleukins antagonist

Cat.No.S2015

Suplatast Tosylate (IPD-1151T, Suplatast Tosilate) is a novel capsular anti-asthmatic agent that suppresses both IgE production, IL-4 and IL-5 synthesis with IC50 above 100 μM.
Suplatast Tosylate Interleukins antagonist Chemical Structure

Chemical Structure

Molecular Weight: 499.64

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Chemical Information, Storage & Stability

Molecular Weight 499.64 Formula

C23H33NO7S2

 Storage (From the date of receipt)
CAS No. 94055-76-2 Download SDF Storage of Stock Solutions

Synonyms IPD-1151T, Suplatast Tosilate Smiles CCOCC(COC1=CC=C(C=C1)NC(=O)CC[S+](C)C)O.CC1=CC=C(C=C1)S(=O)(=O)[O-]

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (200.14 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
IL-4 [1]
(Cell-free assay)
>100 μM
IL-5 [1]
(Cell-free assay)
>100 μM
In vitro
Suplatast tosilate has an inhibitory effect on antibody production in isolated mouse splenic and human peripheral blood B cells with IC50 ＞100 nM. Suplatast tosilate inhibits mouse and human cytokine production, IFN-γ, IL-2, IL-4, IL-5 and IL-10 with an IC50 ＞100 nM. [1] The induction of Cryj1-dependent IgE synthesis mediated by SN-4 is suppressed in a concentration-dependent manner by Suplatast tosilate (1 and 10 µg/ml) in autologous B cells. IL-4 production, both stimulated by SN-4 with Cryj1 in the presence of autologous APC for 3 days and produced by PHA-stimulated PBMC from normal donors, are effectively inhibited in a concentration-dependent manner by Suplatast tosilate (1 and 10 μg/mL). [2] Suplatast tosilate significantly inhibits the expression of CD1a, CD80, and CD86 on immature dendritic cells (DCs) and of CD1a, CD80, CD83, and CD86 on mature DCs. Suplatast tosilate also significantly inhibits the secretion of CCL17, IL-12p70, and IL-12p40; however, the secretion of IL-10 is not affected. The proliferative responses of allogeneic CD4(+) T cells to Suplatast tosilate-treated DCs are suppressed. Moreover, Suplatast tosilate-treated DCs has an impaired capacity to stimulate CD4(+) T cells to produce IFN-gamma and IL-5. [4]
Kinase Assay
ssay for cytokines
The cultures for cytokine production are set up at 37 °C as follows: the mixtures of SN-4 and autologous APC (each 1 × 105 cells/well) are cultured for 3 days with 50 μg/mL of Cry j1 in a total volume of 0.2 mL in round-bottomed micro plates; PBMC (2 × 10 5 cells/well) from normal donors are cultured for 24 hours with 10 μg/ml of PHA in a total volume of 0.2 mL in flat-bottomed, 96-well micro plates; and purified T cells (1 × 105 cells/well) from normal donors are cultured in a total volume of 1 ml for 24 hours with anti-CD3 mAb that have been immobilized on flat-bottomed, 24-well plates at a concentration of 5 µg/ml. Cytokines in the culture supernatants are quantitatively assayed by the following commercially available kits: IL-4 and IFN-γ. The sensitivity of the assay is 30 pg/mL for IL-4 and 1 U/mL for IFN-γ.
In vivo
Suplatast tosilate (100 mg/kg/100 μL) significantly reduces the number of total cells and eosinophils in BALF (around -40%) and almost completely inhibits the development of antigen-induced BHR. Histological findings confirm the reduction of submucosal cell infiltration in the lung, and disclose the marked inhibition of bronchial epithelial cell damage. Ovalbumin-specific IgE is slightly but significantly reduced. The levels of IL-4, IL-5 and IL-13 in BALF are significantly decreased in mice treated with Suplatast tosilate compared to those in untreated mice. [3]
References

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