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Suplatast Tosilate (also known as IPD-1151T) is a novel capsular anti-asthmatic and anti-allergic agent that suppresses both IgE production, IL-4 and IL-5 synthesis with IC50 above 100 μM. 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.
Physicochemical Properties
| Molecular Formula | C23H33NO7S2 | |
| Molecular Weight | 499.64 | |
| Exact Mass | 499.169 | |
| CAS # | 94055-76-2 | |
| Related CAS # | 94055-75-1;94055-76-2; | |
| PubChem CID | 71773 | |
| Appearance | White to off-white solid powder | |
| Melting Point | 84-87ºC | |
| LogP | 3.722 | |
| Hydrogen Bond Donor Count | 2 | |
| Hydrogen Bond Acceptor Count | 7 | |
| Rotatable Bond Count | 10 | |
| Heavy Atom Count | 33 | |
| Complexity | 500 | |
| Defined Atom Stereocenter Count | 0 | |
| InChi Key | RYVJQEZJUFRANT-UHFFFAOYSA-N | |
| InChi Code | 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) | |
| Chemical Name | [3-[4-(3-ethoxy-2-hydroxypropoxy)anilino]-3-oxopropyl]-dimethylsulfanium;4-methylbenzenesulfonate | |
| Synonyms |
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| HS Tariff Code | 2934.99.9001 | |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| ln Vitro | In autologous B cell cultures driven by SN-4, IPD-1151T (1-10 μM; 10 d) produces a concentration-dependent inhibition of purified allergen (Cry j 1)-dependent IgE synthesis, without significantly altering the synthesis of IgG[1]. In normal peripheral blood mononuclear cells (PBMC), IPD-1151T (1-10 μM; 24 h) significantly suppresses the production of IL-4 mRNA produced by phytohemagglutinin (PHA)[1]. |
| ln Vivo | In a murine asthma model, suplatast tosilate (100 mg/kg; once daily for 21 days) suppresses Th2 cytokine production, which in turn suppresses eosinophil infiltration into the murine airway, IgE generation, and development of BHR[2]. One dose every day for 14 days at 100 μg/kg of suplatast tosilate significantly reduces blood immunoglobulin E levels[3]. |
| Animal Protocol |
Animal/Disease Models: Female balb/c (Bagg ALBino) mouse (6-8 weeks old) are immunized with ovalbumin[3] Doses: 100 mg/ kg Route of Administration: Po one time/day for 21 days Experimental Results: decreased the number of total cells and eosinophils. Almost completely inhibited the development of antigen-induced bronchial hyperresponsiveness (BHR). diminished the levels of IL-4, IL-5 and IL- 13. |
| References |
[1]. Suppression of IgE production by IPD-1151T (suplatast tosilate), a new dimethylsulfonium agent: (2). Regulation of human IgE response. Jpn J Pharmacol. 1993 Jan;61(1):31-9. [2]. Effect of suplatast tosilate (IPD-1151T) on a mouse model of asthma: inhibition of eosinophilic inflammation and bronchial hyperresponsiveness. Int Arch Allergy Immunol. 2000 Feb;121(2):116-22. [3]. Suppressive effects of anti-allergic agent suplatast tosilate (IPD-1151T) on the expression of co-stimulatory molecules on mouse splenocytes in vivo. Mediators Inflamm. 2001 Dec;10(6):333-7. [4]. Furonaka M, Hattori N, Tanimoto T, Senoo T, Ishikawa N, Fujitaka K, Haruta Y, Yokoyama A, Kohno N. Suplatast tosilate prevents bleomycin-induced pulmonary fibrosis in mice. J Pharmacol Exp Ther. 2009 Jan;328(1):55-61. |
Solubility Data
| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.00 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (5.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 4: Saline: 30 mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0014 mL | 10.0072 mL | 20.0144 mL | |
| 5 mM | 0.4003 mL | 2.0014 mL | 4.0029 mL | |
| 10 mM | 0.2001 mL | 1.0007 mL | 2.0014 mL |