Methylpiperidinopyrazole
Methylpiperidinopyrazole (MPP) is a synthetic, nonsteroidal, and highly selective antagonist of ERα that is used in scientific research to study the function of this receptor.[1][2] It has 200-fold selectivity for ERα over ERβ and 1000-fold selectivity for blocking ERα-mediated gene transcription relative to that of ERβ.[3]
| ファイル:Methylpiperidinopyrazole.svg | |
|---|---|
| Systematic (IUPAC) name | |
| 4-[2-(4-hydroxyphenyl)-4-methyl-3-[4-(2-piperidin-1-ylethoxy)phenyl]-1H-pyrazol-5-ylidene]cyclohexa-2,5-dien-1-one | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | ? |
| Identifiers | |
| CAS number | 289726-02-9 |
| ATC code | ? |
| PubChem | CID 6604927 |
| ChemSpider | 5037183 |
| Chemical data | |
| Formula | C29H31N3O3 |
| SMILES | eMolecules & PubChem |
| |
See also
- Glyceollin
- Propylpyrazoletriol (PPT)
- Diarylpropionitrile (DPN)
- Prinaberel (ERB-041)
- Liquiritigenin
- Menerba
- PHTPP
- (R,R)-Tetrahydrochrysene ((R,R)-THC)
References
- ↑ Sun J, Huang YR, Harrington WR, Sheng S, Katzenellenbogen JA, Katzenellenbogen BS (March 2002). "Antagonists selective for estrogen receptor alpha". Endocrinology. 143 (3): 941–7. doi:10.1210/endo.143.3.8704. PMID 11861516.
- ↑ Zhou HB, Carlson KE, Stossi F, Katzenellenbogen BS, Katzenellenbogen JA (January 2009). "Analogs of methyl-piperidinopyrazole (MPP): antiestrogens with estrogen receptor alpha selective activity". Bioorganic & Medicinal Chemistry Letters. 19 (1): 108–10. doi:10.1016/j.bmcl.2008.11.006. PMC 2711511. PMID 19014882.
- ↑ Ottow E, Weinmann H (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. 50–. ISBN 978-3-527-62330-3.