TY-51469
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MedKoo CAT#: 555336

CAS#: 603987-59-3

Description: TY-51469 is a Chymase inhibitor TY-51469 in therapy of inflammatory bowel disease. TY-51469 showed IC50s for simian and human chymases of 0.4 and 7.0 nM, respectively. TY-51469 might ameliorate the progression of DSS-induced colitis possibly by increasing the expression of Tregs and cytokines.

Chemical Structure

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TY-51469
CAS# 603987-59-3
Instruction

Theoretical Analysis

MedKoo Cat#: 555336
Name: TY-51469
CAS#: 603987-59-3
Chemical Formula: C20H15FN2O6S4
Exact Mass: 525.98
Molecular Weight: 526.586
Elemental Analysis: C, 45.62; H, 2.87; F, 3.61; N, 5.32; O, 18.23; S, 24.35

Price and Availability

Size Price Availability Quantity
5mg USD 350 2 Weeks
25mg USD 950 2 Weeks
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Synonym: TY-51469; TY 51469; TY51469;

IUPAC/Chemical Name: 2-(4-((5-fluoro-3-methylbenzo[b]thiophene)-2-sulfonamido)-3-(methylsulfonyl)phenyl)thiazole-4-carboxylic acid

InChi Key: CBRCULCCRGSSLB-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H15FN2O6S4/c1-10-13-8-12(21)4-6-16(13)31-20(10)33(28,29)23-14-5-3-11(7-17(14)32(2,26)27)18-22-15(9-30-18)19(24)25/h3-9,23H,1-2H3,(H,24,25)

SMILES Code: O=C(C1=CSC(C2=CC=C(NS(=O)(C3=C(C)C4=CC(F)=CC=C4S3)=O)C(S(=O)(C)=O)=C2)=N1)O

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: >3 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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 526.59 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.

Recalculate based on batch purity %
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:
In vitro protocol:
In vivo protocol:

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1: Chymase inhibitor TY-51469 in therapy of inflammatory bowel disease Wei-Xin Liu, Ying Wang, Li-Xuan Sang, Shen Zhang, Ting Wang, Feng Zhou, Shou-Zhi Gu World J Gastroenterol. 2016 Feb 7; 22(5): 1826–1833. Published online 2016 Feb 7. doi: 10.3748/wjg.v22.i5.1826 PMCID: PMC4724613

2: Pivotal Role of Mouse Mast Cell Protease 4 in the Conversion and Pressor Properties of Big-Endothelin-1 Martin Houde, Marc-David Jamain, Julie Labonté, Louisane Desbiens, Gunnar Pejler, Michael Gurish, Shinji Takai, Pedro D'Orléans-Juste J Pharmacol Exp Ther. 2013 Jul; 346(1): 31–37. Published online 2013 Jul. doi: 10.1124/jpet.112.202275 PMCID: PMC3684843

3: Mouse Mast Cell Protease 4 Deletion Protects Heart Function and Survival After Permanent Myocardial Infarction Martin Houde, Adel Schwertani, Hanène Touil, Louisane Desbiens, Otman Sarrhini, Roger Lecomte, Martin Lepage, Hugo Gagnon, Shinji Takai, Gunnar Pejler, Danielle Jacques, Fernand Gobeil, Jr., Robert Day, Pedro D’Orléans-Juste Front Pharmacol. 2018; 9: 868. Published online 2018 Aug 31. doi: 10.3389/fphar.2018.00868 PMCID: PMC6127244

4: Mast Cells and Wound Healing Carole A. Oskeritzian Adv Wound Care (New Rochelle) 2012 Feb; 1(1): 23–28. doi: 10.1089/wound.2011.0357 PMCID: PMC3623594

5: Mast Cell Chymase and Tryptase as Targets for Cardiovascular and Metabolic Diseases Aina He, Guo-Ping Shi Curr Pharm Des. Author manuscript; available in PMC 2014 Feb 12.Published in final edited form as: Curr Pharm Des. 2013; 19(6): 1114–1125.

PMCID: PMC3921624

6: The emerging role of mast cells in liver disease Veronica Jarido, Lindsey Kennedy, Laura Hargrove, Jennifer Demieville, Joanne Thomson, Kristen Stephenson, Heather Francis Am J Physiol Gastrointest Liver Physiol. 2017 Aug 1; 313(2): G89–G101. Published online 2017 May 4. doi: 10.1152/ajpgi.00333.2016 PMCID: PMC5582878

7: Chymase inhibition as a pharmacological target: a role in inflammatory and functional gastrointestinal disorders? S Heuston, NP Hyland Br J Pharmacol. 2012 Oct; 167(4): 732–740. doi: 10.1111/j.1476-5381.2012.02055.x PMCID: PMC3575774

8: Proteases and Their Inhibitors in Chronic Obstructive Pulmonary Disease Tapan Dey, Jatin Kalita, Sinéad Weldon, Clifford C. Taggart J Clin Med. 2018 Sep; 7(9): 244. Published online 2018 Aug 28. doi: 10.3390/jcm7090244 PMCID: PMC6162857

9: Serotonin Exhibits Accelerated Bleomycin-Induced Pulmonary Fibrosis through TPH1 Knockout Mouse Experiments Jingyao Zhang, Ruixia Cui, Yang Feng, Weiman Gao, Jianbin Bi, Zeyu Li, Chang Liu Mediators Inflamm. 2018; 2018: 7967868. Published online 2018 Apr 16. doi: 10.1155/2018/7967868 PMCID: PMC5926513

10: IL-10-Producing B Cells Suppress Effector T Cells Activation and Promote Regulatory T Cells in Crystalline Silica-Induced Inflammatory Response In Vitro Yiping Lu, Fangwei Liu, Chao Li, Ying Chen, Dong Weng, Jie Chen Mediators Inflamm. 2017; 2017: 8415094. Published online 2017 Aug 2. doi: 10.1155/2017/8415094 PMCID: PMC5558645

11: Biomarkers of the involvement of mast cells, basophils and eosinophils in asthma and allergic diseases Dean D. Metcalfe, Ruby Pawankar, Steven J. Ackerman, Cem Akin, Frederic Clayton, Franco H. Falcone, Gerald J. Gleich, Anne-Marie Irani, Mats W. Johansson, Amy D. Klion, Kristin M. Leiferman, Francesca Levi-Schaffer, Gunnar Nilsson, Yoshimichi Okayama, Calman Prussin, John T. Schroeder, Lawrence B. Schwartz, Hans-Uwe Simon, Andrew F. Walls, Massimo Triggiani World Allergy Organ J. 2016; 9: 7. Published online 2016 Feb 11. doi: 10.1186/s40413-016-0094-3 PMCID: PMC4751725

12: The Importance of Mast Cells in Dermal Scarring Traci A. Wilgus, Brian C. Wulff Adv Wound Care (New Rochelle) 2014 Apr 1; 3(4): 356–365. doi: 10.1089/wound.2013.0457 PMCID: PMC3985512

13: Mast cell activity in the healing wound: More than meets the eye? Brian C. Wulff, Traci A. Wilgus Exp Dermatol. Author manuscript; available in PMC 2014 Aug 1.Published in final edited form as: Exp Dermatol. 2013 Aug; 22(8): 507–510. Published online 2013 Jun 27. doi: 10.1111/exd.12169 PMCID: PMC3723719

14: The diversity of myeloid immune cells shaping wound repair and fibrosis in the lung Laura Florez‐Sampedro, Shanshan Song, Barbro N. Melgert Regeneration (Oxf) 2018 Mar; 5(1): 3–25. Published online 2018 Feb 23. doi: 10.1002/reg2.97 PMCID: PMC5911451

15: Controlling Arteriogenesis and Mast Cells Are Central to Bioengineering Solutions for Critical Bone Defect Repair Using Allografts Ben Antebi, Longze Zhang, Dmitriy Sheyn, Gadi Pelled, Xinping Zhang, Zulma Gazit, Edward M. Schwarz, Dan Gazit Bioengineering (Basel) 2016 Mar; 3(1): 6. Published online 2016 Jan 11. doi: 10.3390/bioengineering3010006 PMCID: PMC4851447

16: Crystalline silica-induced leukotrieneB4-dependent inflammation promotes lung tumor growth Shuchismita R. Satpathy, Venkatakrishna R. Jala, Sobha R. Bodduluri, Elangovan Krishnan, Bindu Hegde, Gary Hoyle, Mostafa Fraig, Andrew D. Luster, Bodduluri Haribabu Nat Commun. 2015; 6: 7064. Published online 2015 Apr 29. doi: 10.1038/ncomms8064 PMCID: PMC4418220

17: Approaches for Analyzing the Roles of Mast Cells and Their Proteases In Vivo Stephen J. Galli, Mindy Tsai, Thomas Marichal, Elena Tchougounova, Laurent L. Reber, Gunnar Pejler Adv Immunol. Author manuscript; available in PMC 2016 Feb 29.Published in final edited form as: Adv Immunol. 2015; 126: 45–127. Published online 2015 Feb 7. doi: 10.1016/bs.ai.2014.11.002 PMCID: PMC4771191

18: Are mast cells instrumental for fibrotic diseases? Catherine Overed-Sayer, Laura Rapley, Tomas Mustelin, Deborah L. Clarke Front Pharmacol. 2013; 4: 174. Published online 2014 Jan 21. doi: 10.3389/fphar.2013.00174 PMCID: PMC3896884

19: The renin angiotensin system and the metabolic syndrome Chih-Hong Wang, Feng Li, Nobuyuki Takahashi Open Hypertens J. Author manuscript; available in PMC 2011 Jan 1.Published in final edited form as: Open Hypertens J. 2010; 3: 1–13. doi: 10.2174/1876526203010001 PMCID: PMC2995894