94055-76-2 Usage
Description
Different sources of media describe the Description of 94055-76-2 differently. You can refer to the following data:
1. 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.
2. 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.
Uses
Different sources of media describe the Uses of 94055-76-2 differently. You can refer to the following data:
1. 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.
2. 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
Check Digit Verification of cas no
The CAS Registry Mumber 94055-76-2 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 9,4,0,5 and 5 respectively; the second part has 2 digits, 7 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 94055-76:
(7*9)+(6*4)+(5*0)+(4*5)+(3*5)+(2*7)+(1*6)=142
142 % 10 = 2
So 94055-76-2 is a valid CAS Registry Number.
InChI:InChI=1/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)
94055-76-2Relevant articles and documents
Four new polymorphic forms of suplatast tosilate
Nagai, Keiko,Ushio, Takanori,Miura, Hidenori,Nakamura, Takashi,Moribe, Kunikazu,Yamamoto, Keiji
, p. 83 - 91 (2014)
We found four new polymorphic forms (γ-, E?-, ζ-, and η-forms) of suplatast tosilate (ST) by recrystallization and seeding with ST-analogous compounds; three polymorphic forms (α-, β-, and δ-forms) of ST have been previously reported. The physicochemical properties of these new forms were investigated using infrared (IR) spectroscopy, solid-state nuclear magnetic resonance (NMR) spectroscopy, differential scanning calorimetry, and powder X-ray diffractometry. The presence of hydrogen bonds in the new forms was assessed from the IR and solid-state NMR spectra. The crystal structures of the E?- and η-forms were determined from their powder X-ray diffraction data using the direct space approach and the Monte Carlo method, followed by Rietveld refinement. The structures determined for the E?- and η-forms supported the presence of hydrogen bonds between the ST molecules, as the IR and solid-state NMR spectra indicated. The thermodynamic characteristics of the seven polymorphic forms were evaluated by determining the solubility of each form. The α-form was the most insoluble in 2-propanol at 35 C, and was thus concluded to be the most stable form. The E?-form was the most soluble, and a polymorphic transition from the E?- to the α-form was observed during solubility testing.
Preparation methods of suplatast tosilate and intermediates
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Paragraph 0017; 0020; 0024, (2018/09/13)
The invention relates to preparation methods of suplatast tosilate and intermediates thereof. According to the method, 4-aminophenol is taken as an initial material, and a target compound is obtainedthrough steps of amidation, addition of epichlorohydrin, ring opening and the like. The method avoids a palladium-carbon catalytic hydrogenation step, comprises a short synthesis route and is high inyield, simple to operate and suitable for industrial application. The invention also provides novel intermediates for preparation of suplatast tosilate and preparation methods of the novel intermediates.
