TCS-5861528 | Chembridge-5861528 | CAS#332117-28-9 | TRPA1 Receptor Antagonist

TCS-5861528
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 522706

CAS#: 332117-28-9

Description: TCS-5861528, also known as Chembridge-5861528, is a TRPA1 receptor antagonist. TCS-5861528 antagonizes AITC- and 4-HNE-evoked calcium influx (IC50 values are 14.3 and 18.7μM respectively). TRPA1 was found to mediate acute inflammation and the development of degenerative cartilage changes and joint pain in MIA-induced experimental OA in the mouse. TRPA1 may be a potential mediator and drug target in OA.

Chemical Structure

TCS-5861528

CAS# 332117-28-9

Instruction

Theoretical Analysis

MedKoo Cat#: 522706
Name: TCS-5861528
CAS#: 332117-28-9
Chemical Formula: C19H23N5O3
Exact Mass: 369.18
Molecular Weight: 369.425
Elemental Analysis: C, 61.77; H, 6.28; N, 18.96; O, 12.99

Price and Availability

Size	Price	Availability
10mg	USD 270	2 Weeks
25mg	USD 490	2 Weeks
50mg	USD 750	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: TCS5861528, TCS-5861528, TCS 5861528, Chembridge-5861528, Chembridge5861528, Chembridge 5861528

IUPAC/Chemical Name: 2-(1,3-Dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-[4-(1-methylpropyl)phenyl]acetamide

InChi Key: ZUTUWJYMCADJHD-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H23N5O3/c1-5-12(2)13-6-8-14(9-7-13)21-15(25)10-24-11-20-17-16(24)18(26)23(4)19(27)22(17)3/h6-9,11-12H,5,10H2,1-4H3,(H,21,25)

SMILES Code: O=C(NC1=CC=C(C(C)CC)C=C1)CN2C=NC(N(C)C(N3C)=O)=C2C3=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, not in water

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:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 369.43 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:
In vitro protocol:
In vivo protocol:

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1: Moilanen LJ, Hämäläinen M, Nummenmaa E, Ilmarinen P, Vuolteenaho K, Nieminen RM, Lehtimäki L, Moilanen E. Monosodium iodoacetate-induced inflammation and joint pain are reduced in TRPA1 deficient mice--potential role of TRPA1 in osteoarthritis. Osteoarthritis Cartilage. 2015 Nov;23(11):2017-26. doi: 10.1016/j.joca.2015.09.008. PubMed PMID: 26521748.

2: Shatillo A, Koroleva K, Giniatullina R, Naumenko N, Slastnikova AA, Aliev RR, Bart G, Atalay M, Gu C, Khazipov R, Davletov B, Grohn O, Giniatullin R. Cortical spreading depression induces oxidative stress in the trigeminal nociceptive system. Neuroscience. 2013 Dec 3;253:341-9. doi:
10.1016/j.neuroscience.2013.09.002. Epub 2013 Sep 11. PubMed PMID: 24036374.

3: Fernandes ES, Vong CT, Quek S, Cheong J, Awal S, Gentry C, Aubdool AA, Liang L, Bodkin JV, Bevan S, Heads R, Brain SD. Superoxide generation and leukocyte accumulation: key elements in the mediation of leukotriene B₄-induced itch by transient receptor potential ankyrin 1 and transient receptor potential vanilloid 1. FASEB J. 2013 Apr;27(4):1664-73. doi: 10.1096/fj.12-221218. Epub 2012 Dec 27. PubMed PMID: 23271050.

4: Vermeulen W, De Man JG, De Schepper HU, Bult H, Moreels TG, Pelckmans PA, DeWinter BY. Role of TRPV1 and TRPA1 in visceral hypersensitivity to colorectal distension during experimental colitis in rats. Eur J Pharmacol. 2013 Jan 5;698(1-3):404-12. doi: 10.1016/j.ejphar.2012.10.014. Epub 2012 Oct 23. PubMed PMID: 23099257.

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TCS-5861528 featured