Suplatast tosylate | Suplatast tosilate | CAS#94055-76-2 | 94055-75-1 | Th2 cytokine inhibitor

MedKoo Cat#: 326795 | Name: Suplatast tosylate

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Suplatast tosylate, also known as Suplatast tosilate, is a Th2 cytokine inhibitor which is used as an antiallergic drug. It is often used in the treatment of Kimura's disease. Suplatast tosylate alleviates nasal symptoms through the suppression of nuclear factor of activated T-cells-mediated IL-9 gene expression in toluene-2,4-diisocyanate-sensitized rats. Suplatast tosylate ameliorates airway hyperreactivity and inflammation through inhibition of the GATA‑3/IL‑5 signaling pathway in asthmatic rats.

Chemical Structure

Suplatast tosylate

CAS#94055-76-2 (tosylate)

Theoretical Analysis

MedKoo Cat#: 326795

Name: Suplatast tosylate

CAS#: 94055-76-2 (tosylate)

Chemical Formula: C23H33NO7S2

Exact Mass: 0.0000

Molecular Weight: 499.64

Elemental Analysis: C, 55.29; H, 6.66; N, 2.80; O, 22.41; S, 12.83

Price and Availability

Size	Price	Availability	Quantity
100mg	USD 450.00
200mg	USD 650.00
500mg	USD 950.00
1g	USD 1,450.00

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Related CAS #

94055-75-1 (free base) 94055-76-2 (tosylate)

Synonym

Suplatast tosilate; Suplatast tosylate.

IUPAC/Chemical Name

(3-((4-(3-ethoxy-2-hydroxypropoxy)phenyl)amino)-3-oxopropyl)dimethylsulfonium 4-methylbenzenesulfonate

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)

SMILES Code

C[S+](CCC(NC1=CC=C(OCC(O)COCC)C=C1)=O)C.CC2=CC=C(S(=O)([O-])=O)C=C2

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Related CAS# CAS#94055-75-1 (Suplatast free base). CAS#94055-76-2 (Suplatast tosylate)

Product Data

Product Data

Instruction

View handling instruction

Biological target:

Suplatast tosilate's biological target is Th2 cytokines, such as interleukin-4 (IL-4) and thymus- and activation-regulated chemokine (TARC). It exerts its anti-allergic effects by inhibiting the production of these cytokines, thereby regulating the immune response associated with allergic reactions.

In vitro activity:

In this in vitro study, suplatast tosilate significantly and dose-dependently inhibited the production of TARC by antigen-specific Th2 cell lines stimulated with relevant antigens or phytohemagglutinin (PHA), demonstrating its ability to suppress Th2 cytokine and chemokine production. These findings suggest that suplatast tosilate could be a useful anti-allergic agent by inhibiting both Th2 cytokines and chemokines. Reference: Oda N, Minoguchi K, Tanaka A, Yokoe T, Minoguchi H, Matsuo H, Nakashima M, Tasaki T, Adachi M. Suplatast tosilate inhibits thymus- and activation-regulated chemokine production by antigen-specific human Th2 cells. Clin Exp Allergy. 2002 Dec;32(12):1782-6.

In vivo activity:

This in vivo study on irradiated mice demonstrated that suplatast tosilate reduced oxidative stress markers and inflammatory cytokine levels in lung tissues, resulting in decreased pulmonary fibrosis and improved survival rates. These findings suggest that suplatast tosilate could serve as a promising lung-protective agent against radiation-induced lung injury during thoracic radiotherapy. Reference: Izumi Y, Nakashima T, Masuda T, Shioya S, Fukuhara K, Yamaguchi K, Sakamoto S, Horimasu Y, Miyamoto S, Iwamoto H, Fujitaka K, Hamada H, Hattori N. Suplatast tosilate reduces radiation-induced lung injury in mice through suppression of oxidative stress. Free Radic Biol Med. 2019 May 20;136:52-59.

	Solvent	mg/mL	mM
Solubility
	Water	100.0	200.10
	DMSO	33.0	66.10

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 499.64 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

Zhou JR, Shirasaki T, Soeda F, Takahama K. Inhibition of suplatast tosilate on EPSC in the single paratracheal ganglion neurons attached with presynaptic boutons. J Neurophysiol. 2023 Jul 1;130(1):56-60. doi: 10.1152/jn.00151.2023. Epub 2023 Jun 7. PMID: 37283483. Izumi Y, Nakashima T, Masuda T, Shioya S, Fukuhara K, Yamaguchi K, Sakamoto S, Horimasu Y, Miyamoto S, Iwamoto H, Fujitaka K, Hamada H, Hattori N. Suplatast tosilate reduces radiation-induced lung injury in mice through suppression of oxidative stress. Free Radic Biol Med. 2019 May 20;136:52-59. doi: 10.1016/j.freeradbiomed.2019.03.024. Epub 2019 Mar 28. PMID: 30930296.

In vitro protocol:

Oda N, Minoguchi K, Tanaka A, Yokoe T, Minoguchi H, Matsuo H, Nakashima M, Tasaki T, Adachi M. Suplatast tosilate inhibits thymus- and activation-regulated chemokine production by antigen-specific human Th2 cells. Clin Exp Allergy. 2002 Dec;32(12):1782-6. doi: 10.1046/j.1365-2222.2002.01547.x. PMID: 12653172. Tanaka A, Minoguchi K, Samson KT, Oda N, Yokoe T, Tazaki T, Yamamoto Y, Yamamoto M, Ohta S, Adachi M. Inhibitory effects of suplatast tosilate on the differentiation and function of monocyte-derived dendritic cells from patients with asthma. Clin Exp Allergy. 2007 Jul;37(7):1083-9. doi: 10.1111/j.1365-2222.2006.02616.x. PMID: 17581203.

In vivo protocol:

1: Mizuguchi H, Orimoto N, Kadota T, Kominami T, Das AK, Sawada A, Tamada M, Miyagi K, Adachi T, Matsumoto M, Kosaka T, Kitamura Y, Takeda N, Fukui H. Suplatast tosilate alleviates nasal symptoms through the suppression of nuclear factor of activated T-cells-mediated IL-9 gene expression in toluene-2,4-diisocyanate-sensitized rats. J Pharmacol Sci. 2016 Mar;130(3):151-8. doi: 10.1016/j.jphs.2015.12.008. Epub 2016 Jan 6. PubMed PMID: 26874672. 2: Fujimoto N, Hamaguchi Y, Tanaka T. Vitiligo-like depigmentation with perifollicular pigment retention in systemic sclerosis treated successfully with suplatast tosilate. Eur J Dermatol. 2016 Feb 1;26(1):110-2. doi: 10.1684/ejd.2015.2687. PubMed PMID: 26841835. 3: Yasudo H, Ando T, Hiwatari M, Oka A. Suplatast tosilate for treating cutaneous mastocytosis. Pediatr Dermatol. 2015 May-Jun;32(3):e118-9. doi: 10.1111/pde.12552. Epub 2015 Mar 17. PubMed PMID: 25779849. 4: Zhou JR, Syono R, Fukumi S, Kimoto K, Shirasaki T, Soeda F, Takahama K. Novel antitussive effect of suplatast tosilate in guinea pigs. Pharmacology. 2015;95(1-2):36-41. doi: 10.1159/000369977. Epub 2015 Jan 13. PubMed PMID: 25592147. 5: Kuramoto T, Senzaki H, Inagaki T. [A case report of eosinophilic cystitis treated with oral suplatast tosilate]. Hinyokika Kiyo. 2014 Sep;60(9):447-50. Japanese. PubMed PMID: 25293800. 6: Liu D, Li Y, Zhong LL, Tan YP. [Effects of suplatast tosilate on airway inflammation and interleukin-5 in asthmatic rats]. Zhongguo Dang Dai Er Ke Za Zhi. 2014 Jul;16(7):759-63. Chinese. PubMed PMID: 25008888. 7: Hashizume H, Umayahara T. Treatment of non-episodic angioedema associated with eosinophilia with suplatast tosilate, an anti-allergic selective Th2 cytokine inhibitor. Eur J Dermatol. 2014 Mar-Apr;24(2):250-2. doi: 10.1684/ejd.2014.2274. PubMed PMID: 24723649. 8: Yoshihara S, Yamada Y, Fukuda H, Tsuchiya T, Ono M, Fukuda N, Kanno N, Arisaka O. Prophylactic effectiveness of suplatast tosilate in children with asthma symptoms in the autumn: a pilot study. Allergol Int. 2014 Jun;63(2):199-203. doi: 10.2332/allergolint.13-OA-0583. Epub 2014 Feb 25. PubMed PMID: 24561769. 9: Nagai K, Ushio T, Miura H, Nakamura T, Moribe K, Yamamoto K. Four new polymorphic forms of suplatast tosilate. Int J Pharm. 2014 Jan 2;460(1-2):83-91. doi: 10.1016/j.ijpharm.2013.10.049. Epub 2013 Nov 6. PubMed PMID: 24211359. 10: Tuncel T, Karaman M, Ayyildiz ZA, Uysal P, Kiray M, Bagriyanik AH, Yilmaz O, Karaman O, Uzuner N. The effects of suplatast tosilate treatment and prophylaxis on lung histopathology in a mouse model of chronic asthma. J Investig Med. 2014 Jan;62(1):56-61. doi: 10.231/JIM.0000000000000012. PubMed PMID: 24113733. 11: Tan Y, Li Y, Liu D, Zhong L. Suplatast tosilate ameliorates airway hyperreactivity and inflammation through inhibition of the GATA 3/IL 5 signaling pathway in asthmatic rats. Mol Med Rep. 2013 Jul;8(1):161-7. doi: 10.3892/mmr.2013.1485. Epub 2013 May 20. PubMed PMID: 23695442. 12: Yoshino T, Moriyama H. Case of eosinophilic cystitis treated with suplatast tosilate as maintenance therapy. Case Rep Urol. 2012;2012:354219. Epub 2012 Sep 11. PubMed PMID: 22997600; PubMed Central PMCID: PMC3446640. 13: Shiga M, Horiguchi T, Kondo R, Miyazaki J, Hirose M, Otake Y, Hata H, Tachikawa S. Long-term monotherapy with suplatast tosilate in patients with mild atopic asthma: a pilot comparison with low-dose inhaled fluticasone. Asian Pac J Allergy Immunol. 2011 Jun;29(2):134-42. PubMed PMID: 21980828. 14: Ueda T, Arai S, Amoh Y, Katsuoka K. Kimura's disease treated with suplatast tosilate and loratadine. Eur J Dermatol. 2011 Nov-Dec;21(6):1020-1. doi: 10.1684/ejd.2011.1539. PubMed PMID: 21914581. 15: Yoshihara S, Fukuda H, Arisaka O. Usefulness of suplatast tosilate, a Th2 cytokine inhibitor based on the Th1/Th2 ratio for allergic disease in children: a retrospective study. Arzneimittelforschung. 2011;61(7):421-4. doi: 10.1055/s-0031-1296221. PubMed PMID: 21899211. 16: Bito T, Kabashima R, Sugita K, Tokura Y. Angiolymphoid hyperplasia with eosinophilia on the leg successfully treated with T-helper cell 2 cytokine inhibitor suplatast tosilate. J Dermatol. 2011 Mar;38(3):300-2. doi: 10.1111/j.1346-8138.2010.00990.x. Epub 2010 Sep 28. PubMed PMID: 21342240. 17: Imashuku S, Ueda I, Inaba T. Effectiveness of a combination of cyclosporine A, suplatast tosilate and prednisolone on periodic oscillating hypereosinophilia. Int Med Case Rep J. 2011 Nov 8;4:79-82. doi: 10.2147/IMCRJ.S26102. Print 2011. PubMed PMID: 23754911; PubMed Central PMCID: PMC3658243. 18: Matsui E, Shinoda S, Fukutomi O, Kaneko H, Fukao T, Kondo N. Relationship between the benefits of suplatast tosilate, a Th2 cytokine inhibitor, and gene polymorphisms in children with bronchial asthma. Exp Ther Med. 2010 Nov;1(6):977-982. Epub 2010 Sep 15. PubMed PMID: 22993628; PubMed Central PMCID: PMC3445962. 19: Bae SJ, Lee JB, Shimizu K, Kuwazuka Y. Increase effect of transforming growth factor on eotaxin production by normal cultured dermal fibroblasts stimulated with interleukin-4: inhibitory effect of suplatast tosilate on eotaxin production. Immunol Invest. 2010 Jan;39(2):93-102. doi: 10.3109/08820130903496769. PubMed PMID: 20136617. 20: Watanabe M, Yamaguchi K, Yamanishi T, Kamai T, Yoshida K. [A case of eosinophilic cystitis that was treated with oral suplatast tosilate (IPD-1151T)]. Hinyokika Kiyo. 2009 Nov;55(11):715-9. Japanese. PubMed PMID: 19946192.