Suplatast TosylateTh2 cytokine synthesis inhibitor; antiasthmatic CAS# 94055-76-2 |
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Quality Control & MSDS
3D structure
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| Cas No. | 94055-76-2 | SDF | Download SDF |
| PubChem ID | 71773 | Appearance | Powder |
| Formula | C23H33NO7S2 | M.Wt | 499.64 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | IPD 1151T | ||
| Solubility | DMSO : ≥ 33 mg/mL (66.05 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | [3-[[4-(3-Ethoxy-2-hydroxypropoxy)p | ||
| SMILES | CCOCC(COC1=CC=C(C=C1)NC(=O)CC[S+](C)C)O.CC1=CC=C(C=C1)S(=O)(=O)[O-] | ||
| Standard InChIKey | RYVJQEZJUFRANT-UHFFFAOYSA-N | ||
| Standard 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) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | 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. |
Suplatast Tosylate Dilution Calculator
Suplatast Tosylate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.0014 mL | 10.0072 mL | 20.0144 mL | 40.0288 mL | 50.036 mL |
| 5 mM | 0.4003 mL | 2.0014 mL | 4.0029 mL | 8.0058 mL | 10.0072 mL |
| 10 mM | 0.2001 mL | 1.0007 mL | 2.0014 mL | 4.0029 mL | 5.0036 mL |
| 50 mM | 0.04 mL | 0.2001 mL | 0.4003 mL | 0.8006 mL | 1.0007 mL |
| 100 mM | 0.02 mL | 0.1001 mL | 0.2001 mL | 0.4003 mL | 0.5004 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Suplatast Tosilate(IPD 1151T) is a Th2 cytokine inhibitor that attenuates IL-2, IL-5 and IL-13 production and has no effect on IFN-γ production.
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Simultaneous inhibition of T helper 2 and T regulatory cell differentiation by small molecules enhances Bacillus Calmette-Guerin vaccine efficacy against tuberculosis.[Pubmed:25315774]
J Biol Chem. 2014 Nov 28;289(48):33404-11.
Tuberculosis affects nine million individuals and kills almost two million people every year. The only vaccine available, Bacillus Calmette-Guerin (BCG), has been used since its inception in 1921. Although BCG induces host-protective T helper 1 (Th1) cell immune responses, which play a central role in host protection, its efficacy is unsatisfactory, suggesting that additional methods to enhance protective immune responses are needed. Recently we have shown that simultaneous inhibition of Th2 cells and Tregs by using the pharmacological inhibitors Suplatast Tosylate and D4476, respectively, dramatically enhances Mycobacterium tuberculosis clearance and induces superior Th1 responses. Here we show that treatment with these two drugs during BCG vaccination dramatically improves vaccine efficacy. Furthermore, we demonstrate that these drugs induce a shift in the development of T cell memory, favoring central memory T (Tcm) cell responses over effector memory T (Tem) cell responses. Collectively, our findings provide evidence that simultaneous inhibition of Th2 cells and Tregs during BCG vaccination promotes vaccine efficacy.
Suplatast tosilate prevents bleomycin-induced pulmonary fibrosis in mice.[Pubmed:18832650]
J Pharmacol Exp Ther. 2009 Jan;328(1):55-61.
Increasing evidence suggests that the development of pulmonary fibrosis is a T helper (Th) 2-mediated process. Suplatast tosilate is a Th2 cytokine inhibitor that is widely used as an asthma controller in Japan. Therefore, we hypothesized that suplatast tosilate might have an inhibitory effect on the development of pulmonary fibrosis. To investigate this effect, suplatast tosilate was administered to mice after the intratracheal instillation of bleomycin (BLM). The effect of suplatast tosilate was studied by analysis of bronchoalveolar lavage (BAL) fluid and a hydroxyproline assay. We found that the treatment of mice with suplatast tosilate significantly reduced the degree of pulmonary fibrosis. Because a significantly elevated Th2 response was not detected in the C57BL/6 mice after BLM administration, the effect of suplatast tosilate on Th2 cytokines could not be demonstrated. Interestingly, however, the up-regulation of the monocyte chemoattractant protein (MCP)-1 levels in the BAL fluid was found to be suppressed. Following these results, we also demonstrated that suplatast tosilate effectively inhibited the production of MCP-1 in alveolar macrophages (AMs). These findings suggest that suplatast tosilate has both anti-inflammatory and antifibrotic effects, which were associated with a suppressed MCP-1 expression in AMs. Thus, suplatast tosilate, which is already widely used in Japan, may warrant further consideration as a potentially useful treatment for pulmonary fibrosis.
The effects of suplatast tosilate (IPD-1151T) on innate immunity and antigen-presenting cells.[Pubmed:18005853]
Transpl Immunol. 2007 Nov;18(2):108-14.
We previously demonstrated that the anti-allergic drug, suplatast tosilate (IPD-1151T), prolonged rat survival after heterotopic heart transplantation (HHT) and suppressed mixed lymphocyte reaction (MLR). In the present study, we investigated the effects of suplatast on T cells, lipopolysaccharides (LPS), or peptidoglycan (PGN)-stimulated cells and dendritic cells (DCs). The addition of suplatast to concanavalin A (ConA) blasts inhibited the proliferation of cells in which the gene expression of T-helper-1 (Th1) and T-helper-2 (Th2) cytokines including interferon (IFN)-gamma, interleukin (IL)-2, IL-4, and IL-10 were down-regulated with decreased concentration of the IFN-gamma and IL-10 in the supernatants of ConA blast cells. Suplatast also showed down-regulation of the toll-like receptor (TLR)2, TLR4, and CD14 gene expressions on splenocytes stimulated by LPS and PGN, TLR2 or TLR4 agonist, respectively. DCs treated with suplatast expressed lower levels of CD40, CD80, and CD86 and reduced IL-12 production. These results suggest that suplatast may modulate the TLRs on antigen-presenting cells (APCs) and thus block the pathway of Th1/Th2 cytokine production.
Suppressive effects of anti-allergic agent suplatast tosilate (IPD-1151T) on the expression of co-stimulatory molecules on mouse splenocytes in vivo.[Pubmed:11817674]
Mediators Inflamm. 2001 Dec;10(6):333-7.
The effects of IPD-1151T on the expression of co-stimulatory molecules, CD40, CD80 and CD86, were investigated in vivo using mice with allergic disorders. BALB/c mice were immunized intraperitoneally with two doses of dinitrophenylated ovalbumin (DNP-OVA) at 1-week intervals. These mice then were treated intraperitoneally with 100 microg/kg of IPD-1151T once a day for 14 days, starting 7 days after the first immunization. On day 21, some mice were challenged intraperitoneally with DNP-OVA and the other mice were not challenged. All mice were autopsied on day 22 and assayed for immunoglobulin E, interleuken (IL)-4 and IL-5 productions following DNP-OVA immunization. The intraperitoneal treatment with IPD-1151T strongly suppressed immunoglobulin E contents in serum, which were enhanced by DNA-OVA immunization. IPD-1151T also caused a decrease in both IL-4 and IL-5 levels in splenic lymphocytes. We next examined the influence of IPD-1151T on co-stimulatory molecule expression on splenic lymphocytes. IPD-1151T caused suppression of CD40 and CD86 expression; however, the treatments did not affect CD80 expression.
