5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDE
5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDE Basic information
- Product Name:
- 5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDE
- Synonyms:
-
- 5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDE
- AG 045572
- 2-Furancarboxamide, 5-[(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)methyl]-N-(2,4,6-trimethoxyphenyl)-
- CAS:
- 263847-55-8
- MF:
- C30H37NO5
- MW:
- 491.62
- Mol File:
- 263847-55-8.mol
5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDE Chemical Properties
- storage temp.
- Store at RT
- solubility
- <49.16mg/ml in DMSO; <24.58mg/ml in ethanol
- form
- solid
- color
- White
5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDE Usage And Synthesis
Uses
AG 045572 is a nonpeptidic GnRH antagonist and has the potential as an oral therapeutic treatement for sex hormone-dependent diseases and infertility.
Biological Activity
Selective gonadotropin-releasing hormone (GnRH) receptor antagonist (K i values are 2.2, 3.8 and 6.0 nM for mouse, rat and human receptors respectively). Suppresses testosterone and luteinising hormone (LH) levels in vivo .
References
[1]. barnes mj, burschka c, büttner mw, et al. silicon analogues of the nonpeptidic gnrh antagonist ag-045572: syntheses, crystal structure analyses, and pharmacological characterization. chemmedchem, 2011, 6(11): 2070-2080.
[2]. zhu yf, chen c, struthers rs. nonpeptide gonadotropin releasing hormone antagonists. annu. rep. med. chem, 2004, 39(99): 110.
[3]. anderes kl, luthin dr, castillo r, et al. biological characterization of a novel, orally active small molecule gonadotropin-releasing hormone (gnrh) antagonist using castrated and intact rats. journal of pharmacology and experimental therapeutics, 2003, 305(2): 688-695.
[4]. herbst kl. gonadotropin-releasing hormone antagonists. current opinion in pharmacology, 2003, 3(6): 660-666.
5-[5,6,7,8-TETRAHYDRO-3,5,5,8,8-PENTAMETHYL-2-NAPHTHALENYL-METHYL]-N-(2,4,6-TRIMETHOXYPHENYL)-2-FURANCARBOXAMIDESupplier
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