RU-59063 (original) (raw)
RU-59063 is a nonsteroidal androgen or selective androgen receptor modulator (SARM) which was first described in 1994 and was never marketed. It was originally thought to be a potent antiandrogen, but subsequent research found that it actually possesses dose-dependent androgenic activity, albeit with lower efficacy than dihydrotestosterone (DHT). The drug is an N-substituted arylthiohydantoin and was derived from the first-generation nonsteroidal antiandrogen (NSAA) nilutamide. The second-generation NSAAs enzalutamide, RD-162, and apalutamide were derived from RU-59063.
| Property | Value |
|---|---|
| dbo:abstract | RU-59063 is a nonsteroidal androgen or selective androgen receptor modulator (SARM) which was first described in 1994 and was never marketed. It was originally thought to be a potent antiandrogen, but subsequent research found that it actually possesses dose-dependent androgenic activity, albeit with lower efficacy than dihydrotestosterone (DHT). The drug is an N-substituted arylthiohydantoin and was derived from the first-generation nonsteroidal antiandrogen (NSAA) nilutamide. The second-generation NSAAs enzalutamide, RD-162, and apalutamide were derived from RU-59063. RU-59063 has high affinity for the human androgen receptor (AR) (Ki = 2.2 nM; Ka = 5.4 nM) and 1,000-fold selectivity for the AR over other nuclear steroid hormone receptors, including the PR, ER, GR, and MR. It shows 3- and 8-fold higher affinity than testosterone for the rat and human AR, respectively, and up to 100-fold higher affinity for the rat AR than the first-generation NSAAs flutamide, nilutamide, and bicalutamide. It also has slightly higher affinity for the AR than DHT and nearly equal affinity to that of the very-high-affinity AR ligand metribolone (R-1881). In addition, RU-59063, unlike testosterone and DHT, shows no specific binding to human plasma. (en) |
| dbo:casNumber | 155180-53-3 |
| dbo:chEMBL | 331820 |
| dbo:class | dbr:Selective_androgen_receptor_modulator dbr:Nonsteroidal_androgen |
| dbo:pubchem | 197655 |
| dbo:thumbnail | wiki-commons:Special:FilePath/RU-59063.svg?width=300 |
| dbo:wikiPageExternalLink | https://wi-doc.com/ https://www.99sarms.com/mk677.html/ https://www.melanotanexpress.com/product/mk-677-25mg-per-ml-30ml-bottle/ |
| dbo:wikiPageID | 56054658 (xsd:integer) |
| dbo:wikiPageLength | 6483 (xsd:nonNegativeInteger) |
| dbo:wikiPageRevisionID | 1124439419 (xsd:integer) |
| dbo:wikiPageWikiLink | dbr:Potency_(pharmacology) dbr:Nuclear_receptor dbr:Bicalutamide dbr:Blood_plasma dbr:Androgen dbr:Androgen_receptor dbc:Imidazolidines dbr:Hydantoin dbc:Abandoned_drugs dbc:Ketones dbc:Primary_alcohols dbc:Thioureas dbc:Trifluoromethyl_compounds dbr:Enzalutamide dbr:Antiandrogen dbr:Apalutamide dbr:Cyanonilutamide dbr:Flutamide dbr:Nilutamide dbr:Nonsteroidal dbc:Nitriles dbr:Testosterone dbc:Selective_androgen_receptor_modulators dbr:Affinity_(pharmacology) dbr:Binding_selectivity dbr:Efficacy dbr:Thio- dbr:Dihydrotestosterone dbr:Metribolone dbr:RD-162 dbr:RU-58642 dbr:RU-58841 dbr:Selective_androgen_receptor_modulator dbr:Steroid_hormone_receptor dbr:Plasma_protein_binding dbr:Nonsteroidal_antiandrogen dbr:Substituent dbr:Nonsteroidal_androgen dbr:Aryl_group |
| dbp:c | 17 (xsd:integer) |
| dbp:casNumber | 155180 (xsd:integer) |
| dbp:chembl | 331820 (xsd:integer) |
| dbp:chemspiderid | 171095 (xsd:integer) |
| dbp:class | dbr:Selective_androgen_receptor_modulator dbr:Nonsteroidal_androgen |
| dbp:f | 3 (xsd:integer) |
| dbp:h | 18 (xsd:integer) |
| dbp:iupacName | 4 (xsd:integer) |
| dbp:n | 3 (xsd:integer) |
| dbp:o | 2 (xsd:integer) |
| dbp:pubchem | 197655 (xsd:integer) |
| dbp:s | 1 (xsd:integer) |
| dbp:smiles | CC1C (en) |
| dbp:stdinchi | 1 (xsd:integer) |
| dbp:stdinchikey | FIDNKDVRTLFETI-UHFFFAOYSA-N (en) |
| dbp:width | 250 (xsd:integer) |
| dbp:wikiPageUsesTemplate | dbt:Androgen_receptor_modulators dbt:Drugbox dbt:Genito-urinary-drug-stub dbt:Reflist dbt:Abbrlink |
| dct:subject | dbc:Imidazolidines dbc:Abandoned_drugs dbc:Ketones dbc:Primary_alcohols dbc:Thioureas dbc:Trifluoromethyl_compounds dbc:Nitriles dbc:Selective_androgen_receptor_modulators |
| rdf:type | owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q8386 dbo:Drug |
| rdfs:comment | RU-59063 is a nonsteroidal androgen or selective androgen receptor modulator (SARM) which was first described in 1994 and was never marketed. It was originally thought to be a potent antiandrogen, but subsequent research found that it actually possesses dose-dependent androgenic activity, albeit with lower efficacy than dihydrotestosterone (DHT). The drug is an N-substituted arylthiohydantoin and was derived from the first-generation nonsteroidal antiandrogen (NSAA) nilutamide. The second-generation NSAAs enzalutamide, RD-162, and apalutamide were derived from RU-59063. (en) |
| rdfs:label | RU-59063 (en) |
| owl:sameAs | wikidata:RU-59063 dbpedia-tr:RU-59063 https://global.dbpedia.org/id/4XCbx |
| prov:wasDerivedFrom | wikipedia-en:RU-59063?oldid=1124439419&ns=0 |
| foaf:depiction | wiki-commons:Special:FilePath/RU-59063.svg |
| foaf:isPrimaryTopicOf | wikipedia-en:RU-59063 |
| is dbo:wikiPageRedirects of | dbr:RU-59,063 dbr:RU59063 dbr:RU_59,063 dbr:RU_59063 |
| is dbo:wikiPageWikiLink of | dbr:RU-56187 dbr:Enzalutamide dbr:Apalutamide dbr:Cyanonilutamide dbr:RD-162 dbr:RU-57073 dbr:RU-58642 dbr:RU-58841 dbr:RU-59,063 dbr:RU59063 dbr:RU_59,063 dbr:RU_59063 |
| is foaf:primaryTopic of | wikipedia-en:RU-59063 |
