Suplatast tosylate

Suplatast tosylate, also known as Suplatast tosilate, is a Th2 cytokine inhibitor which is used as an antiallergic drug. Often used in the treatment of Kimura's disease. Suplatast tosilate alleviates nasal symptoms through the suppression of nuclear factor of activated T-cells-mediated IL-9 gene expression in toluene-2, 4-diisocyanate-sensitized rats. uplatast tosilate ameliorates airway hyperreactivity and inflammation through inhibition of the GATA‑3/IL‑5 signaling pathway in asthmatic rats.

Product information

CAS Number: 94055-76-2

Molecular Weight: 499.64

Formula: C23H33NO7S2

Synonym:

Suplatast tosilate

Related CAS Number:

94055-75-1 (Suplatast free base)

Chemical Name: (3-((4-(3-ethoxy-2-hydroxypropoxy)phenyl)amino)-3-oxopropyl)dimethylsulfonium 4-methylbenzenesulfonate

Smiles: CC1C=CC(=CC=1)S([O-])(=O)=O.CCOCC(O)COC1C=CC(=CC=1)NC(=O)CC[S+](C)C

InChiKey: RYVJQEZJUFRANT-UHFFFAOYSA-N

InChi: InChI=1S/C16H25NO4S.C7H8O3S/c1-4-20-11-14(18)12-21-15-7-5-13(6-8-15)17-16(19)9-10-22(2)3;1-6-2-4-7(5-3-6)11(8,9)10/h5-8,14,18H,4,9-12H2,1-3H3;2-5H,1H3,(H,8,9,10)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 100 mg/mL(200.14 mM). Water: 100 mg/mL(200.14 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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). 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.

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.

References:

1. Zhao GD, et al. Int Arch Allergy Immunol, 2000, 121(2), 116-122.
2. Yanagihara Y, et al. Jpn J Pharmacol, 1993, 61(1), 31-39.
3. Mimura T, et al. J Pharmacol Exp Ther, 2005, 314(1), 293-301.

Products are for research use only. Not for human use.