Chemistry:NNC 45-0095
From HandWiki
Short description: Chemical compound
 | |
| Clinical data | |
|---|---|
| Other names | NNC-450095 |
| Drug class | Selective estrogen receptor modulator |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| ChEMBL | |
| Chemical and physical data | |
| Formula | C18H15NO |
| Molar mass | 261.324 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
NC 45-0095 is a synthetic nonsteroidal selective estrogen receptor modulator (SERM) which was under development by Novo Nordisk for the treatment of postmenopausal osteoporosis but was never marketed.[1][2][3][4][5] It is a partial agonist of the estrogen receptor (IC50 (for binding inhibition) = 9.5 nM; EC50 = 13 nM) with mixed estrogenic and antiestrogenic activity, and shows full estrogenic activity in bone and uterus (Emax (relative to moxestrol, in Ishikawa endometrial cancer cell line) = 105%).[1][4] The compound is a pyrroloindolizine derivative.[1][2] Its development was discontinued by 2003.[5]
See also
References
- ↑ 1.0 1.1 1.2 "Synthesis and pharmacology of a novel pyrrolo[2,1,5-cd] indolizine (NNC 45-0095), a high affinity non-steroidal agonist for the estrogen receptor". Bioorganic & Medicinal Chemistry Letters 10 (4): 399–402. February 2000. doi:10.1016/S0960-894X(00)00015-9. PMID 10714509.
- ↑ 2.0 2.1 "Indolizine: a biologically active moiety". Medicinal Chemistry Research 23 (8): 3593–3606. 2014. doi:10.1007/s00044-014-0940-1. ISSN 1054-2523.
- ↑ "Estrogen receptor modulators: relationships of ligand structure, receptor affinity and functional activity". Current Topics in Medicinal Chemistry 3 (14): 1663–1682. 2003. doi:10.2174/1568026033451727. PMID 14683521.
- ↑ 4.0 4.1 "Understanding the Molecular Mechanism of Action of Estrogen Receptor Modulators. Frontiers in Medicinal Chemistry-Online". Frontiers in Medicinal Chemistry. 2. Bentham Science Publishers. January 2005. pp. 183-231 (206). ISBN 978-1-60805-205-9. https://books.google.com/books?id=tCyDoIHToBQC&pg=PA206.
- ↑ 5.0 5.1 "NNC 450095". AdisInsight. Springer Nature Switzerland AG. https://adisinsight.springer.com/drugs/800014610.
 |  |
