Suplatast tosilate Chemical Properties

Melting point:

84-87°C

storage temp. 

Inert atmosphere,Room Temperature

solubility 

DMSO: >20mg/mL

form 

powder

color 

white to off-white

Merck 

14,9003

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months.

CAS DataBase Reference

94055-76-2(CAS DataBase Reference)

Safety Information

WGK Germany 

3

RTECS 

WR7906000

HS Code 

2930.90.2900

Toxicity

LD50 in male, female mice, male, female rats (mg/kg): 81, 96, 96, 93 i.v.; in mice, rats (g/kg): >12.5, >10 orally (Yamashita)

Suplatast tosilate Usage And Synthesis

Description

Suplatast tosylate is a unique dimethylsulfonium salt marketed in Japan for the treatment of bronchial asthma, atopic dermatitis and allergic rhinitis. Suplatast tosylate is a potent inhibitor of IgE synthesis without suppressing IgM and IgG. The mechanism of action for suplatast tosylate is thought to be via the inhibition of interleukin-4 and interleukin-6 production by T-cells at the gene level. In allergic patients, suplatast tosylate markedly improved clinical symptoms which correlated with a significant decrease in serum IgE antibody levels.

Description

Suplatast is an antiallergic agent. It inhibits IL-4 and IL-5 production in conalbumin-stimulated D10.G4.1 murine T helper 2 (Th2) cells in a concentration-dependent manner. Suplatast (100 mg/kg) inhibits ovalbumin-induced increases in eosinophil and total cell numbers, as well as IL-4, IL-5, and IL-13, but not IFN-γ, levels in bronchoalveolar lavage fluid (BALF) in an ovalbumin-sensitized mouse model of asthma. It also inhibits ovalbumin-induced increases in ovalbumin-specific IgE in serum and bronchial hyperresponsiveness to methacholine in the ovalbumin-sensitized mouse model of asthma.

Originator

Taiho (Japan)

Uses

Suplatast Tosylate is an antiallergic drug. Suplatast Tosylate inhibits antigen-induced histamine release from mast cells as well as IgE antibody formation. Suplatast Tosylate suppresses interleukin (IL)-4 release from T cells, however in human peripheral basophils, Suplatast Tosylate inhibited the antigen-induced release of IL-13 but not IL-4.

Uses

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.

brand name

IPD

Biological Activity

Th2 cytokine inhibitor that attenuates IL-2, IL-5 and IL-13 production and has no effect on IFN- γ production. Acts as an immunoregulator that suppresses IgE production, eosinophil infiltration and histamine release. Exhibits antiasthmatic, anti-inflammatory and antifibrotic activity in vivo and is orally active.

References

1) Kurokawa?et al.?(2001),?Suppressive effects of anti-allergic agent suplatast tosilate (IPD-1151T) on the expression of co-stimulatory molecules on mouse splenocytes in vivo; Mediators Inflamm.,?10?333 2) Hsu?et al.?(2007),?The effects of suplatast tosilate (IPD-1151T) on innate immunity and antigen-presenting cells; Transpl. Immunol.,?18?108 3) Furonaka?et al.?(2009),?Suplatast tosilate prevents bleomycin-induced pulmonary fibrosis in mice; Curr. Opin. J. Pharmacol. Exp. Ther.,?328?55 4) Bhattachrya?et al.?(2014),?Simultaneous inhibition of T helper 2 and T regulatory cell differentiation by small molecules enhances Bacillus Calmette-Guerin vaccine efficacy against tuberculosis; J. Biol. Chem.,?289?33404 5) Wada?et al.?(2009),?Effect of suplatast tosilate on antileukotriene non-responders with mild-to-moderate persistent asthma; Allergol. Int.,?58?389

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