T-5224
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MedKoo CAT#: 206216

CAS#: 530141-72-1

Description: T-5224 is a selective inhibitor of c-Fos/activator protein-1. T-5224 ameliorates liver injury and improves survival through decreasing production of proinflammatory cytokines and chemokines in endotoxemic mice. T-5224 has been investigated in phase II human clinical trials. T-5224 may be a promising new treatment for septic kidney injury. Activator protein 1 (AP-1) is a pivotal transcription factor that regulates a wide range of cellular processes including proliferation, apoptosis, differentiation, survival, cell migration, and transformation.


Chemical Structure

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T-5224
CAS# 530141-72-1

Theoretical Analysis

MedKoo Cat#: 206216
Name: T-5224
CAS#: 530141-72-1
Chemical Formula: C29H27NO8
Exact Mass: 517.17367
Molecular Weight: 517.52658
Elemental Analysis: C, 67.30; H, 5.26; N, 2.71; O, 24.73

Size Price Shipping out time Quantity
10mg USD 150 Same day
25mg USD 250 Same day
50mg USD 450 Same day
100mg USD 750 Same day
200mg USD 1250 Same day
500mg USD 2150 Same day
1g USD 3450 Same day
2g USD 5850 Same day
5g USD 9850 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-07. Prices are subject to change without notice.

T-5224, purity > 98%, is in stock. The same day shipping out after order is received.

Synonym: T5224, T-5224, T 5224

IUPAC/Chemical Name: 3-(5-(4-(cyclopentyloxy)-2-hydroxybenzoyl)-2-((3-hydroxybenzo[d]isoxazol-6-yl)methoxy)phenyl)propanoic acid

InChi Key: DALCQQSLNPLQFZ-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H27NO8/c31-24-15-21(37-20-3-1-2-4-20)8-10-22(24)28(34)19-6-11-25(18(14-19)7-12-27(32)33)36-16-17-5-9-23-26(13-17)38-30-29(23)35/h5-6,8-11,13-15,20,31H,1-4,7,12,16H2,(H,30,35)(H,32,33)

SMILES Code: O=C(O)CCC1=CC(C(C2=CC=C(OC3CCCC3)C=C2O)=O)=CC=C1OCC4=CC5=C(C=C4)C(O)=NO5

Appearance:
White to off-white crystalline solid

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

Preparing Stock Solutions

The following data is based on the product molecular weight 517.52658 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.

Select a batch to recalculate based on the batch molecular weight:
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

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1: Ye N, Ding Y, Wild C, Shen Q, Zhou J. Small Molecule Inhibitors Targeting Activator Protein 1 (AP-1). J Med Chem. 2014 Aug 28;57(16):6930-48. doi: 10.1021/jm5004733. Epub 2014 May 27. PubMed PMID: 24831826; PubMed Central PMCID: PMC4148154.

2: Miyazaki H, Morishita J, Ueki M, Nishina K, Shiozawa S, Maekawa N. The effects of a selective inhibitor of c-Fos/activator protein-1 on endotoxin-induced acute kidney injury in mice. BMC Nephrol. 2012 Nov 23;13:153. doi: 10.1186/1471-2369-13-153. PubMed PMID: 23173923; PubMed Central PMCID: PMC3557146.

3: Izuta S, Ueki M, Ueno M, Nishina K, Shiozawa S, Maekawa N. T-5224, a selective inhibitor of c-Fos/activator protein-1, attenuates lipopolysaccharide-induced liver injury in mice. Biotechnol Lett. 2012 Dec;34(12):2175-82. doi: 10.1007/s10529-012-1022-4. Epub 2012 Aug 25. PubMed PMID: 22927112.

4: Avouac J, Palumbo K, Tomcik M, Zerr P, Dees C, Horn A, Maurer B, Akhmetshina A, Beyer C, Sadowski A, Schneider H, Shiozawa S, Distler O, Schett G, Allanore Y, Distler JH. Inhibition of activator protein 1 signaling abrogates transforming growth factor β-mediated activation of fibroblasts and prevents experimental fibrosis. Arthritis Rheum. 2012 May;64(5):1642-52. doi: 10.1002/art.33501. PubMed PMID: 22139817.

5: Uchihashi S, Fukumoto H, Onoda M, Hayakawa H, Ikushiro S, Sakaki T. Metabolism of the c-Fos/activator protein-1 inhibitor T-5224 by multiple human UDP-glucuronosyltransferase isoforms. Drug Metab Dispos. 2011 May;39(5):803-13. doi: 10.1124/dmd.110.037952. Epub 2011 Feb 23. PubMed PMID: 21346002.