SB-218078（Cat No.:I009313）is a selective antagonist of the neurokinin-1 (NK1) receptor, primarily researched for its potential in managing conditions associated with pain and inflammation. By blocking the NK1 receptor, SB-218078 may reduce the effects of substance P, a neuropeptide involved in pain signaling and emotional responses. This compound has shown promise in preclinical studies for alleviating chronic pain and anxiety-related disorders. Its specificity for the NK1 receptor makes it an intriguing candidate for further investigation in drug development aimed at improving therapeutic outcomes in pain management and related disorders.
| Catalog Number | I009313 |
| CAS Number | 135897-06-2 |
| Synonyms | SB218078; SB218078; SB218078.;(5R,8S)-7,8-dihydro-5H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacene-13,15(6H,14H)-dione |
| Molecular Formula | C24H15N3O3 |
| Purity | ≥95% |
| Target | Chk |
| Solubility | Soluble in DMSO, not in water |
| Storage | Store at -20°C |
| IUPAC Name | 28-oxa-4,14,19-triazaoctacyclo[12.11.2.115,18.02,6.07,27.08,13.019,26.020,25]octacosa-1,6,8,10,12,20,22,24,26-nonaene-3,5-dione |
| InChI | InChI=1S/C24H15N3O3/c28-23-19-17-11-5-1-3-7-13(11)26-15-9-10-16(30-15)27-14-8-4-2-6-12(14)18(22(27)21(17)26)20(19)24(29)25-23/h1-8,15-16H,9-10H2,(H,25,28,29) |
| InChIKey | OTPNDVKVEAIXTI-UHFFFAOYSA-N |
| SMILES | C1CC2N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N(C1O2)C7=C53)C(=O)NC6=O |
| Reference | </br>1:Jennings-Gee J, Pardee TS, Gmeiner WH. Replication-dependent irreversible topoisomerase 1 poisoning is responsible for FdUMP[10] anti-leukemic activity. Exp Hematol. 2013 Feb;41(2):180-188.e4. doi: 10.1016/j.exphem.2012.10.007. Epub 2012 Oct 17. PubMed PMID: 23085462; PubMed Central PMCID: PMC3660094.</br>2:Park JH, Kim WS, Kim JY, Park MH, Nam JH, Yun CW, Kwon YG, Jo I. Chk1 and Hsp90 cooperatively regulate phosphorylation of endothelial nitric oxide synthase at serine 1179. Free Radic Biol Med. 2011 Dec 15;51(12):2217-26. doi: 10.1016/j.freeradbiomed.2011.09.021. Epub 2011 Sep 25. PubMed PMID: 22001744. |
