化合物T-5224
T-5224(T-5224)
CAS: 530141-72-1
化学式: C29H27NO8
| 中文名 | T-5224 |
| 英文名 | T-5224 |
| 别名 | 化合物T-5224 3-(5-(4-(环戊基氧基)-2-羟基苯甲酰基)-2-((3-羟基-1,2-苯并异恶唑-6-基)甲氧基)苯基)丙酸 |
| 英文别名 | T5224 T-5225 T-5224 CS-1217 T 5224. 3-(5-(4-(Cyclopentyloxy)-2-hydroxybenzoyl)-2-((3-hydroxybenzo-[d]isoxazol-6-yl)methoxy)phenyl) 3-(5-(4-(Cyclopentyloxy)-2-hydroxybenzoyl)-2-((3-oxo-2,3-dihydrobenzo[d]isoxazol-6-yl)methoxy) 3-[5-[4-(cyclopentoxy)-2-hydroxy-benzoyl]-2-[(3-hydroxy-1,2-benzo xazol-6-yl)methoxy]phenyl]propanoic acid Benzenepropanoic acid, 5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(2,3-dihydro-3-oxo-1,2-benzisoxazol-6-yl)Methoxy]- |
| CAS | 530141-72-1 |
| 化学式 | C29H27NO8 |
| 分子量 | 517.53 |
| 密度 | 1.376±0.06 g/cm3(Predicted) |
| 溶解度 | DMSO: ≥ 31 mg/mL |
| 酸度系数 | 4.61±0.10(Predicted) |
| 存储条件 | -20℃ |
| 靶点 | c-Fos/AP-1 |
| 参考资料 展开查看 | 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.1 |
化合物T-5224 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.932 ml | 9.661 ml | 19.323 ml |
| 5 mM | 0.386 ml | 1.932 ml | 3.865 ml |
| 10 mM | 0.193 ml | 0.966 ml | 1.932 ml |
| 5 mM | 0.039 ml | 0.193 ml | 0.386 ml |
最后更新：2024-01-02 23:10:35
化合物T-5224 - 细胞实验
NIH/3T3 cells were transiently transfected with the luciferase reporter plasmids pAP-1-Luc (× 7 TGACTAA), pNF-kB-Luc (× 5 TGGGGACTTTCCGC) or control phRL-TK, and cultured overnight. Cells were incubated in 0.5% FBS/DMEM containing T-5224 for 1 h, and then stimulated with PMA (10 ng/ml) or TNFa (10 ng/ml), and then cultured for 3 h, followed by measurement of lysate by using dual-luciferase reporter assay system.
最后更新：2023-08-16 21:32:38
化合物T-5224 - 动物实验
Mice were housed in an SPF (specific pathogen-free) grade environment and provided food and water ad libitum with a 12 h:12 h light/dark cycle. Male 8-week-old DBA/1J mice were immunized with bovine type II collagen emulsified in Freund’s complete adjuvant on days 0 and 21. T-5224, MTX and LEF were orally administered once per day. Arthritis was assessed in a blind fashion for four paws per mouse using the following score: 0, uninvolved; 1, swelling of ≤2 toes or slight swelling in ankles and wrists; 2, swelling of ≥3 toes or moderate swelling in ankles and wrists; 3, extensive swelling of total paw. X-ray films of four paws taken using Softex were assessed for joint destruction in 2nd to 5th proximal interphalangeal joints and five metatarsophalangeal joints of four paws, the carpal joints of the forepaws, and the tarsal and calcaneal joints of the hind paws. Score was: 0, no change; 1, partial erosion; 2, complete erosion for joints; and 0, negative; 0.5, positive for osteoporosis. IL-1β (500 ng per unilate
最后更新：2023-08-16 21:32:38
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