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Suplatast Tosylate

Name: Suplatast Tosylate
Brand: Selleck Chemicals
SKU: S2015
Rating: 5 (1 reviews)

Synonyms: IPD-1151T, Suplatast Tosilate

Catalog No.S2015 Purity:99.98%

Suplatast Tosylate (IPD-1151T, 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.

Suplatast Tosylate Chemical Structure

CAS No. 94055-76-2

Purity & Quality Control

Batch: Purity: 99.98%

99.98

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Biological Activity

Description

Suplatast Tosylate (IPD-1151T, 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.

Targets

IL-4 ^[1] (Cell-free assay)	IL-5 ^[1] (Cell-free assay)
>100 μM	>100 μM

In vitro
In vitro	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. ^[1] 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. IL-4 production, both stimulated by SN-4 with Cryj1 in the presence of autologous APC for 3 days and produced by PHA-stimulated PBMC from normal donors, are effectively inhibited in a concentration-dependent manner by Suplatast tosilate (1 and 10 μg/mL). ^[2] Suplatast tosilate significantly inhibits the expression of CD1a, CD80, and CD86 on immature dendritic cells (DCs) and of CD1a, CD80, CD83, and CD86 on mature DCs. Suplatast tosilate also significantly inhibits the secretion of CCL17, IL-12p70, and IL-12p40; however, the secretion of IL-10 is not affected. The proliferative responses of allogeneic CD4(+) T cells to Suplatast tosilate-treated DCs are suppressed. Moreover, Suplatast tosilate-treated DCs has an impaired capacity to stimulate CD4(+) T cells to produce IFN-gamma and IL-5. ^[4]
Kinase Assay	ssay for cytokines
Kinase Assay	The cultures for cytokine production are set up at 37 °C as follows: the mixtures of SN-4 and autologous APC (each 1 × 10⁵ cells/well) are cultured for 3 days with 50 μg/mL of Cry j1 in a total volume of 0.2 mL in round-bottomed micro plates; PBMC (2 × 10 ⁵ cells/well) from normal donors are cultured for 24 hours with 10 μg/ml of PHA in a total volume of 0.2 mL in flat-bottomed, 96-well micro plates; and purified T cells (1 × 10⁵ cells/well) from normal donors are cultured in a total volume of 1 ml for 24 hours with anti-CD3 mAb that have been immobilized on flat-bottomed, 24-well plates at a concentration of 5 µg/ml. Cytokines in the culture supernatants are quantitatively assayed by the following commercially available kits: IL-4 and IFN-γ. The sensitivity of the assay is 30 pg/mL for IL-4 and 1 U/mL for IFN-γ.
Cell Research	Cell lines	Dendritic cells (DCs) and CD4+ T cells
	Concentrations	10 or 100 μg/mL
	Incubation Time	5 days
	Method	Allogeneic responder CD4+ T cells obtained from healthy subjects are purified from PBMCs by negative depletion of CD14+, CD16+, CD19+, CD56+, and CD8+ cells using magnetic cell separation system micro-beads and columns. After 7 days of culture with GM-CSF and IL-4, iDCs differentiated from monocytes in the presence or absence of Suplatast tosilate (10 and 100 mg/ mL) are co-cultured with purified 1×10 ⁵ allogeneic CD41 T cells at varying ratios of iDCs in 96-well round bottomed culture plates for 5 days. Cells are pulsed with 1 μCi of ³H-methylthymidine for the last 8 hours of the culture period. Incorporated radioactivity is counted with a liquid scintillation counter, and proliferative responses are expressed as the mean ³ H-methylthymidine incorporation (counts per minutes) of triplicate wells_SEM. Proliferation of DCs alone or CD4+ T cells alone is also assessed.

In Vivo
In vivo	Suplatast tosilate (100 mg/kg/100 μL) significantly reduces the number of total cells and eosinophils in BALF (around -40%) and almost completely inhibits the development of antigen-induced BHR. Histological findings confirm the reduction of submucosal cell infiltration in the lung, and disclose the marked inhibition of bronchial epithelial cell damage. Ovalbumin-specific IgE is slightly but significantly reduced. The levels of IL-4, IL-5 and IL-13 in BALF are significantly decreased in mice treated with Suplatast tosilate compared to those in untreated mice. ^[3]
Animal Research	Animal Models	BALB/c mice sensitized to ovalbumin
	Dosages	100 mg/kg/100 μL
	Administration	Orally once a day for 21 days

References

[4] Tanaka A, et al. Clin Exp Allergy, 2007, 37(7), 1083-1089.

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Chemical Information & Solubility

Molecular Weight	499.64	Formula	C₂₃H₃₃NO₇S₂
CAS No.	94055-76-2	SDF	Download Suplatast Tosylate SDF
Smiles	CCOCC(COC1=CC=C(C=C1)NC(=O)CC[S+](C)C)O.CC1=CC=C(C=C1)S(=O)(=O)[O-]
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (200.14 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Clear solution	saline	100.000mg/ml (200.14mM)	Taking the 1 mL working solution as an example, add 100 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	saline	99.000mg/ml (198.14mM)	Taking the 1 mL working solution as an example, add 99 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	saline	100.000mg/ml (200.14mM)	Taking the 1 mL working solution as an example, add 100 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	Saline Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (60.04mM)	Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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