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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
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.
| Targets |
B cell IgE synthesis pathway [1]
- T cell/B cell co-stimulatory molecules (CD80, CD86) [3] - Cytokine signaling pathways (IL-4, IFN-γ, TGF-β) [1, 4] |
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| 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].
Inhibited IgE production by human peripheral blood mononuclear cells (PBMCs) stimulated with pokeweed mitogen (PWM) in a concentration-dependent manner: 100 μg/mL Suplatast Tosylate (IPD 1151T) reduced IgE secretion by ~60% compared to vehicle control [1] - Regulated cytokine balance in human PBMCs: 100 μg/mL concentration decreased IL-4 (pro-allergic cytokine) production by ~45% and increased IFN-γ (anti-allergic cytokine) production by ~55% [1] - Did not affect PBMC viability at concentrations up to 200 μg/mL (trypan blue staining, cell survival rate > 90%) [1] - Suppressed LPS-induced upregulation of CD80 and CD86 expression on mouse splenocytes by ~40% and ~35%, respectively, at 100 μg/mL [3] |
| 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].
In a BALB/c mouse ovalbumin (OVA)-induced asthma model, oral administration of Suplatast Tosylate (IPD 1151T) (100, 300 mg/kg/day for 14 days) dose-dependently inhibited eosinophilic inflammation in the lung [2] - 300 mg/kg dose reduced bronchoalveolar lavage fluid (BALF) eosinophil count by ~70% and decreased serum OVA-specific IgE levels by ~50% [2] - Attenuated bronchial hyperresponsiveness (BHR) to methacholine: 300 mg/kg reduced airway resistance by ~45% compared to vehicle control [2] - In C57BL/6 mice, oral Suplatast Tosylate (IPD 1151T) (300 mg/kg/day for 7 days) suppressed CD80 and CD86 expression on splenic B cells and dendritic cells by ~35-40% [3] - In a mouse bleomycin-induced pulmonary fibrosis model, oral administration (300 mg/kg/day for 21 days) starting 1 day after bleomycin injection reduced lung collagen deposition by ~60% and decreased TGF-β1 mRNA expression by ~55% [4] - Improved lung function: reduced lung hydroxyproline content (a marker of collagen) by ~50% and alleviated alveolar wall thickening [4] |
| Cell Assay |
Human PBMC IgE secretion assay: Human PBMCs were isolated from healthy donors and seeded in 24-well plates. Cells were treated with Suplatast Tosylate (IPD 1151T) (10-200 μg/mL) and stimulated with PWM (10 μg/mL) for 14 days. Culture supernatants were collected, and IgE concentration was quantified by ELISA. IL-4 and IFN-γ levels were also measured by ELISA [1]
- Mouse splenocyte co-stimulatory molecule assay: Splenocytes were isolated from C57BL/6 mice and cultured in 6-well plates. Cells were treated with Suplatast Tosylate (IPD 1151T) (10-100 μg/mL) and stimulated with LPS (1 μg/mL) for 24 hours. CD80 and CD86 expression on B cells and dendritic cells was detected by flow cytometry using specific antibodies [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. Mouse OVA-induced asthma model: 6-week-old BALB/c mice were sensitized with OVA + aluminum hydroxide by intraperitoneal injection on days 0 and 7. From day 14 to 27, mice were challenged with OVA aerosol (1% OVA in saline) for 30 minutes daily. Suplatast Tosylate (IPD 1151T) was suspended in 0.5% carboxymethylcellulose and administered orally at 100 or 300 mg/kg/day from day 14 to 27. On day 28, mice were euthanized; BALF was collected for cell counting, serum for OVA-specific IgE detection, and lungs for histological analysis [2] - Mouse splenocyte co-stimulatory molecule regulation model: 8-week-old C57BL/6 mice were administered Suplatast Tosylate (IPD 1151T) (300 mg/kg/day) orally for 7 days. Splenocytes were isolated, and CD80/CD86 expression was analyzed by flow cytometry. Control mice received vehicle alone [3] - Mouse bleomycin-induced pulmonary fibrosis model: 8-week-old C57BL/6 mice were anesthetized and administered bleomycin (3.5 U/kg) via intratracheal injection. Suplatast Tosylate (IPD 1151T) (300 mg/kg/day) was given orally from day 1 to 21 post-bleomycin. On day 21, mice were euthanized; lungs were collected for hydroxyproline assay, collagen staining (Masson's trichrome), and TGF-β1 mRNA quantification by RT-PCR [4] |
| Toxicity/Toxicokinetics |
In vitro cytotoxicity: At concentrations up to 200 μg/mL, no significant toxicity was observed in human peripheral blood mononuclear cells (PBMCs) or mouse spleen cells [1, 3]
- In vivo toxicity: In mice, no significant adverse reactions (weight loss, behavioral abnormalities) were observed after daily doses up to 300 mg/kg for 21 consecutive days. Serum ALT, AST, and creatinine levels were not significantly different from those in the solvent control group [2, 4] - Human clinical tolerability: No serious adverse events were reported in the preliminary studies; mild gastrointestinal discomfort (≤5% of subjects) was transient [1] |
| References |
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| Additional Infomation |
Suplatast Tosylate (IPD 1151T) is a novel dimethylsulfonium drug with anti-allergic and anti-inflammatory activities [1, 2, 3, 4]. Its core mechanisms include: 1) inhibiting B cell IgE synthesis by regulating the IL-4/IFN-γ balance; 2) inhibiting the expression of co-stimulatory molecules (CD80/CD86) to attenuate T cell activation; and 3) inhibiting pro-fibrotic cytokine (TGF-β1) to prevent tissue fibrosis [1, 3, 4]. Potential therapeutic indications include allergic asthma, allergic rhinitis, atopic dermatitis, and pulmonary fibrosis [2, 4]. Its good oral bioavailability and long-term tolerability make it suitable for the treatment of chronic inflammatory/allergic diseases [2, 4]. Unlike traditional antihistamines, it targets the root cause of allergies (IgE production and immune cell activation) rather than relieving symptoms [1, 2].
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| Molecular Formula |
C23H33NO7S2
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| Molecular Weight |
499.64
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| Exact Mass |
499.169
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| CAS # |
94055-76-2
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| Related CAS # |
94055-75-1;94055-76-2;
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| PubChem CID |
71773
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| Appearance |
White to off-white solid powder
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| Melting Point |
84-87ºC
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| LogP |
3.722
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
33
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| Complexity |
500
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RYVJQEZJUFRANT-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
[3-[4-(3-ethoxy-2-hydroxypropoxy)anilino]-3-oxopropyl]-dimethylsulfanium;4-methylbenzenesulfonate
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| 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)
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| 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. View More
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. Solubility in Formulation 4: Saline: 30 mg/mL |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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