Resatorvid
Resatorvid, also known as TAK-242, is a cell-permeable inhibitor of TLR4 signaling, blocking LPS-induced production of NO, TNF-α, IL-6, and IL-1β in macrophages with IC50 values of 1-11 nM. Resatorvid binds selectively to TLR4 and interferes with interactions between TLR4 and its adaptor molecules. Resatorvid provides neuroprotection in experimental traumatic brain injury: implication in the treatment of human brain injury.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | Resatorvid |
|---|---|
| Iupac 化学名称 | ethyl (R)-6-(N-(2-chloro-4-fluorophenyl)sulfamoyl)cyclohex-1-ene-1-carboxylate |
| 同义词 | TAK-242; TAK 242; TAK242; Resatorvid |
| 英文同义词 | TAK-242; TAK 242; TAK242; Resatorvid |
| 分子式 | C15H17ClFNO4S |
| 分子量 | 361.8124 |
| Smile | FC1=CC(Cl)=C(NS([C@@H]2CCCC=C2C(OCC)=O)(=O)=O)C=C1 |
| InChiKey | LEEIJTHMHDMWLJ-CQSZACIVSA-N |
| InChi | InChI=1S/C15H17ClFNO4S/c1-2-22-15(19)11-5-3-4-6-14(11)23(20,21)18-13-8-7-10(17)9-12(13)16/h5,7-9,14,18H,2-4,6H2,1H3/t14-/m1/s1 |
| Cas号 | 243984-11-4 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 干燥、黑暗，短期（日至周）0-4摄氏度，长期（月至年）0-20摄氏度。 |
| 可溶性 | 可溶于DMSO |
| 处理方式 | |
| 运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周。 |
| 海关编码 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Feng Y, Gao J, Cui Y, Li M, Li R, Cui C, Cui J. Neuroprotective Effects of
Resatorvid Against Traumatic Brain Injury in Rat: Involvement of Neuronal
Autophagy and TLR4 Signaling Pathway. Cell Mol Neurobiol. 2016 Mar 10. [Epub
ahead of print] PubMed PMID: 26961544.
2: Zhang D, Li H, Li T, Zhou M, Hao S, Yan H, Yu Z, Li W, Li K, Hang C. TLR4
inhibitor resatorvid provides neuroprotection in experimental traumatic brain
injury: implication in the treatment of human brain injury. Neurochem Int. 2014
Sep;75:11-8. doi: 10.1016/j.neuint.2014.05.003. Epub 2014 May 20. PubMed PMID:
24858944.
3: Takeuchi T, Jinno F, Ebihara T, Moriya Y, Kadotani R, Tagawa Y, Kondo T, Itoh
T, Asahi S. Species differences of organic anion transporters involved in the
renal uptake of 4-amino-3-chlorophenyl hydrogen sulfate, a metabolite of
resatorvid, between rats and dogs. Biopharm Drug Dispos. 2013 May;34(4):236-46.
doi: 10.1002/bdd.1841. Epub 2013 May 7. PubMed PMID: 23529922.
4: Jinno F, Takeuchi T, Tagawa Y, Kondo T, Itoh T, Asahi S. Differences in the
pharmacokinetics of 4-amino-3-chlorophenyl hydrogen sulfate, a metabolite of
resatorvid, in rats and dogs. Drug Metab Dispos. 2012 Apr;40(4):648-54. doi:
10.1124/dmd.111.043729. Epub 2011 Dec 27. PubMed PMID: 22203697.
5: Matsunaga N, Tsuchimori N, Matsumoto T, Ii M. TAK-242 (resatorvid), a
small-molecule inhibitor of Toll-like receptor (TLR) 4 signaling, binds
selectively to TLR4 and interferes with interactions between TLR4 and its adaptor
molecules. Mol Pharmacol. 2011 Jan;79(1):34-41. doi: 10.1124/mol.110.068064. Epub
2010 Sep 29. PubMed PMID: 20881006.
