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]

Methylpiperidinopyrazole
Identifiers
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
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
FormulaC29H31N3O3
Molar mass469.585 g·mol−1
3D model (JSmol)
SMILES
  • CC1=C(N(NC1=C2C=CC(=O)C=C2)C3=CC=C(C=C3)O)C4=CC=C(C=C4)OCCN5CCCCC5
InChI
  • InChI=1S/C29H31N3O3/c1-21-28(22-5-11-25(33)12-6-22)30-32(24-9-13-26(34)14-10-24)29(21)23-7-15-27(16-8-23)35-20-19-31-17-3-2-4-18-31/h5-16,30,34H,2-4,17-20H2,1H3
  • Key:PFTIONINVMINHE-UHFFFAOYSA-N

See also

References
  1. 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.
  2. 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.
  3. Ottow E, Weinmann H (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. 50–. ISBN 978-3-527-62330-3.
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