ERA-45

ERA-45
Clinical data
Drug class	Estrogen; Selective ERα agonist
Identifiers
CAS Number	1044260-74-3
PubChem SID	472218960

ERA-45 is a synthetic estrogen and a selective agonist of the ERα.^[1]^[2]^[3]^[4] It shows 286-fold selectivity for transactivation of the ERα over the ERβ, with EC₅₀ values of 0.37 nM for the ERα (7-fold weaker than estradiol) and 13 nM for the ERβ (20,000-fold weaker than estradiol).^[1] However, another found only about 35-fold potency for transactivation of the ERα over the ERβ.^[2] The drug has no antagonistic activity at either receptor.^[1] ERA-45 induced prostate cancer development in preclinical models when it was given in combination with testosterone, whereas testosterone alone did not do so.^[1]^[5] In contrast, the selective ERβ agonist ERB-26 was protective against the development of prostate cancer produced by these two drugs.^[1]^[5] These findings suggest opposing roles of the ERα and ERβ in the prostate gland.^[1] The chemical structure of ERa-45 does not appear to have been disclosed.

References

^ ^a ^b ^c ^d ^e ^f Attia DM, Ederveen AG (2012). "Opposing roles of ERα and ERβ in the genesis and progression of adenocarcinoma in the rat ventral prostate". Prostate. 72 (9): 1013–22. doi:10.1002/pros.21507. PMID 22025007. S2CID 12951793.
^ ^a ^b Jeanes HL, Tabor C, Black D, Ederveen A, Gray GA (2008). "Oestrogen-mediated cardioprotection following ischaemia and reperfusion is mimicked by an oestrogen receptor (ER)α agonist and unaffected by an ER beta antagonist". J. Endocrinol. 197 (3): 493–501. doi:10.1677/JOE-08-0071. PMC 2386536. PMID 18492815.
^ Evers NM, van den Berg JH, Wang S, Melchers D, Houtman R, de Haan LH, Ederveen AG, Groten JP, Rietjens IM (2014). "Cell proliferation and modulation of interaction of estrogen receptors with coregulators induced by ERα and ERβ agonists". J. Steroid Biochem. Mol. Biol. 143: 376–85. doi:10.1016/j.jsbmb.2014.06.002. PMID 24923734. S2CID 9884692.
^ Khalil RA (2013). "Estrogen, vascular estrogen receptor and hormone therapy in postmenopausal vascular disease". Biochem. Pharmacol. 86 (12): 1627–42. doi:10.1016/j.bcp.2013.09.024. PMC 3840081. PMID 24099797.
^ ^a ^b Nelson AW, Tilley WD, Neal DE, Carroll JS (2014). "Estrogen receptor beta in prostate cancer: friend or foe?". Endocr. Relat. Cancer. 21 (4): T219–34. doi:10.1530/ERC-13-0508. PMID 24402043.

Estrogen receptor modulators

Agonists	Steroidal: 2-Hydroxyestradiol 2-Hydroxyestrone 3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol 3α-Androstanediol 3α,5α-Dihydrolevonorgestrel 3β,5α-Dihydrolevonorgestrel 3α-Hydroxytibolone 3β-Hydroxytibolone 3β-Androstanediol 4-Androstenediol 4-Androstenedione 4-Fluoroestradiol 4-Hydroxyestradiol 4-Hydroxyestrone 4-Methoxyestradiol 4-Methoxyestrone 5-Androstenediol 7-Oxo-DHEA 7α-Hydroxy-DHEA 7α-Methylestradiol 7β-Hydroxyepiandrosterone 8,9-Dehydroestradiol 8,9-Dehydroestrone 8β-VE2 10β,17β-Dihydroxyestra-1,4-dien-3-one (DHED) 11β-Chloromethylestradiol 11β-Methoxyestradiol 15α-Hydroxyestradiol 16-Ketoestradiol 16-Ketoestrone 16α-Fluoroestradiol 16α-Hydroxy-DHEA 16α-Hydroxyestrone 16α-Iodoestradiol 16α-LE2 16β-Hydroxyestrone 16β,17α-Epiestriol (16β-hydroxy-17α-estradiol) 17α-Estradiol (alfatradiol) 17α-Dihydroequilenin 17α-Dihydroequilin 17α-Epiestriol (16α-hydroxy-17α-estradiol) 17α-Ethynyl-3α-androstanediol 17α-Ethynyl-3β-androstanediol 17β-Dihydroequilenin 17β-Dihydroequilin 17β-Methyl-17α-dihydroequilenin Abiraterone Abiraterone acetate Alestramustine Almestrone Anabolic steroids (e.g., testosterone and esters, methyltestosterone, metandienone (methandrostenolone), nandrolone and esters, many others; via estrogenic metabolites) Atrimustine Bolandiol Bolandiol dipropionate Butolame Clomestrone Cloxestradiol Cloxestradiol acetate Conjugated estriol Conjugated estrogens Cyclodiol Cyclotriol DHEA DHEA-S ent-Estradiol Epiestriol (16β-epiestriol, 16β-hydroxy-17β-estradiol) Epimestrol Equilenin Equilin ERA-63 (ORG-37663) Esterified estrogens Estetrol Estradiol Estradiol esters Lipoidal estradiol Polyestradiol phosphate Estramustine Estramustine phosphate Estrapronicate Estrazinol Estriol Estriol esters Polyestriol phosphate Estrofurate Estrogenic substances Estromustine Estrone Estrone esters Estrone methyl ether Estropipate Etamestrol (eptamestrol) Ethinylandrostenediol Ethandrostate Ethinylestradiol Ethinylestradiol 3-benzoate Ethinylestradiol sulfonate Ethinylestriol Ethylestradiol Etynodiol Etynodiol diacetate Hexolame Hippulin Hydroxyestrone diacetate Lynestrenol Lynestrenol phenylpropionate Mestranol Methylestradiol Moxestrol Mytatrienediol Nilestriol Norethisterone Noretynodrel Orestrate Pentolame Prodiame Prolame Promestriene RU-16117 Quinestradol Quinestrol Tibolone Nonsteroidal: (R,R)-THC (S,S)-THC 2,8-DHHHC β-LGND1 β-LGND2 (GTx-878) AC-186 Allenestrol Allenolic acid Benzestrol Bifluranol Bisdehydrodoisynolic acid Butestrol Carbestrol D-15414 DCW234 Diarylpropionitrile Dienestrol Dienestrol diacetate Diethylstilbestrol Diethylstilbestrol esters Dimestrol (dianisylhexene) Dimethylstilbestrol Doisynoestrol (fenocycline) Doisynolic acid Efavirenz Elacestrant ERB-196 (WAY-202196) Erteberel (SERBA-1, LY-500307) Estrobin (DBE) Fenestrel FERb 033 Fosfestrol (diethylstilbestrol diphosphate) Furostilbestrol (diethylstilbestrol difuroate) GTx-758 Hexestrol Hexestrol esters ICI-85966 (Stilbostat) M2613 meso-Butestrol meso-Hexestrol Mestilbol Methallenestril Methestrol Methestrol dipropionate Paroxypropione Pentafluranol Phenestrol Prinaberel (ERB-041, WAY-202041) Propylpyrazoletriol Quadrosilan SC-3296 SC-4289 SERBA-2 SKF-82,958 Terfluranol Triphenylbromoethylene Triphenylchloroethylene Triphenyliodoethylene Triphenylmethylethylene (triphenylpropene) WAY-166818 WAY-169916 WAY-200070 WAY-204688 (SIM-688) WAY-214156 Unknown/unsorted: ERB-26 ERA-45 ERB-79 ZK-283197 Xenoestrogens: Anise-related (e.g., anethole, anol, dianethole, dianol, photoanethole) Chalconoids (e.g., isoliquiritigenin, phloretin, phlorizin (phloridzin), wedelolactone) Coumestans (e.g., coumestrol, psoralidin) Flavonoids (incl. 7,8-DHF, 8-prenylnaringenin, apigenin, baicalein, baicalin, biochanin A, calycosin, catechin, daidzein, daidzin, ECG, EGCG, epicatechin, equol, formononetin, glabrene, glabridin, genistein, genistin, glycitein, kaempferol, liquiritigenin, mirificin, myricetin, naringenin, penduletin, pinocembrin, prunetin, puerarin, quercetin, tectoridin, tectorigenin) Lavender oil Lignans (e.g., enterodiol, enterolactone, nyasol (cis-hinokiresinol)) Metalloestrogens (e.g., cadmium) Pesticides (e.g., alternariol, dieldrin, endosulfan, fenarimol, HPTE, methiocarb, methoxychlor, triclocarban, triclosan) Phytosteroids (e.g., digitoxin (digitalis), diosgenin, guggulsterone) Phytosterols (e.g., β-sitosterol, campesterol, stigmasterol) Resorcylic acid lactones (e.g., zearalanone, α-zearalenol, β-zearalenol, zearalenone, zeranol (α-zearalanol), taleranol (teranol, β-zearalanol)) Steroid-like (e.g., deoxymiroestrol, miroestrol) Stilbenoids (e.g., resveratrol, rhaponticin) Synthetic xenoestrogens (e.g., alkylphenols, bisphenols (e.g., BPA, BPF, BPS), DDT, parabens, PBBs, PHBA, phthalates, PCBs) Others (e.g., agnuside, rotundifuran)
Mixed (SERMsTooltip Selective estrogen receptor modulators)	2-Phenylbenzofuran 2-Phenylbenzothiophene 4'-Hydroxynorendoxifen 27-Hydroxycholesterol Acefluranol Acolbifene Afimoxifene Anordiol Anordrin Arzoxifene Bazedoxifene Brilanestrant Broparestrol Camizestrant Chlorotrianisene Clomifene Clomifenoxide CN-55945-27 Cyclofenil D-15413 Desmethylchlorotrianisene Droloxifene Enclomifene Endoxifen Etacstil (GW-5638, DPC-974) Ethamoxytriphetol (MER-25) Femarelle Fispemifene GW-7604 ICI-55548 Idoxifene Lasofoxifene Levormeloxifene LN-1643 LN-2299 LY-117018 Menerba Miproxifene Miproxifene phosphate MRL-37 Nafoxidine Nitromifene NNC 45-0095 NNC 45-0320 NNC 45-0781 NNC 45-1506 Ormeloxifene Ospemifene Panomifene Pipendoxifene Promensil Raloxifene Rimostil (P-081) Spironolactone SS1010 Tamoxifen TAS-108 (SR-16234) Toremifene Trioxifene TZE-5323 U-11555A U-11634 Y-134 Zindoxifene Zuclomifene
Antagonists	(R,R)-THC 7β-Hydroxy-DHEA Chloroindazole Cytestrol acetate EM-800 (SCH-57050) Epitiostanol ERA-90 ERB-88 Fulvestrant (ICI-182780) Glyceollins (I, II, III, IV) ICI-164384 MDL-101906 Mepitiostane Methylepitiostanol Methylpiperidinopyrazole MIBE Oxabicycloheptene sulfonate Phenytoin PHTPP Prochloraz RU-39411 RU-58668 SS1020 TAS-108 (SR-16234) ZB716 ZK-164015 ZK-191703 Coregulator-binding modulators: ERX-11 Noncompetitive inhibitors: Trilostane

GPER

Agonists	2-Methoxyestradiol 7β-Hydroxyepiandrosterone Afimoxifene (4-hydroxytamoxifen) Aldosterone Atrazine Bisphenol A Daidzein DDT (p,p'-DDT, o',p'-DDE) Diarylpropionitrile Equol Estradiol Ethinylestradiol Fulvestrant (ICI-182780) G-1 Genistein GPER-L1 GPER-L2 Hydroxytyrosol Kepone Nicotinic acid Nicotinamide Nonylphenol Oleuropein PCBs (2,2',5'-PCB-4-OH) Propylpyrazoletriol Quercetin Raloxifene Resveratrol STX Tamoxifen Tectoridin
Antagonists	CCL18 Estriol G-15 G-36 MIBE
Unknown	Diethylstilbestrol Zearalenone

See also: Receptor/signaling modulators; Estrogens and antiestrogens; Androgen receptor modulators; Progesterone receptor modulators; List of estrogens

This drug article relating to the genito-urinary system is a stub. You can help Wikipedia by expanding it.

Read other articles:

Akhmad Fauzi Aseri

Akhmad Fauzi AseriLahir23 Desember 1955 (umur 68)Angkinang, Hulu Sungai Selatan, Kalimantan SelatanKebangsaanIndonesiaPekerjaanPengajarDikenal atasGuru Besar dan Rektor IAIN Antasari Prof. Dr. H. Akhmad Fauzi Aseri, M.A. (lahir 23 Desember 1955) adalah seorang pakar di bidang pendidikan Islam dan pengajar Indonesia. Ia menjabat sebagai rektor IAIN Antasari periode 2009 hingga 2017.[1] Pendidikan S0 (B.A) Fakultas Syariah IAIN Antasari cabang Kandangan (1978) S1 (Drs) Jurusan Taf...

Federica Pellegrini

Federica Pellegrini Pellegrini nel 2009 Nazionalità Italia Altezza 179 cm Peso 65 kg Nuoto Specialità Stile libero, dorso Termine carriera 2022 Record 100 m s.l. 5318 (2016) 200 m s.l. 1'5298 (2009) 400 m s.l. 3'5915 (2009) 800 m s.l. 8'2499 (2010) Carriera Squadre di club DDS Milano Circolo Canottieri Aniene 2019-2021 Aqua Centurions11 (166) Nazionale Italia Palmarès Competizione Ori Argenti Bronzi Giochi olimpici 1 1 0 Mondiali 6 4 1 Mondiali in vasca corta 1 2 5 Europei 7 6 ...

Quicksand (TV series)

Swedish TV series or program QuicksandSwedishStörst av allt Genre Crime drama Teen drama Thriller Created by Pontus Edgren Martina Håkansson Based onQuicksand(Störst av allt)by Malin Persson GiolitoWritten byCamilla AhlgrenDirected byPer-Olav Sørensen Lisa Farzaneh Starring Hanna Ardéhn Felix Sandman William Spetz Ella Rappich David Dencik Reuben Sallmander Maria Sundbom Rebecka Hemse Arvid Sand Helena af Sandeberg Anna Björk ComposerKristian Eidnes AndersenCountry of originSwedenOrigi...

Uganda

Republik UgandaRepublic of Uganda (Inggris)Jamhuri ya Uganda (Swahili) Bendera Lambang Semboyan: For God and My Country (Untuk Tuhan dan Negaraku)Lagu kebangsaan: Oh Uganda, Land of Beauty Ibu kota(dan kota terbesar)Kampala00°18′49″N 32°34′52″E / 0.31361°N 32.58111°E / 0.31361; 32.58111Bahasa resmiInggris dan SwahiliPemerintahanRepublik semi-presidensial• Presiden Yoweri Museveni• Perdana Menteri Ruhakana Rugunda LegislatifParlemenKe...

Stuart Smalley

Fictional character created by Al Franken Stuart Smalley Stuart Smalley is a fictional character created and performed by comedian and satirist Al Franken. The character originated on the television show Saturday Night Live, in a mock self-help show called Daily Affirmations With Stuart Smalley. It first aired on the show's February 9, 1991 episode hosted by Kevin Bacon. Stuart is Franken's middle name.[1] Franken has stated that his going to Al-Anon meetings inspired [the character] ...

Ke Lingling

First wife of Xi Jinping Ke LinglingBorn1951 (age 72–73)Puning, GuangdongSpouse Xi Jinping (m. 1979; div. 1982)ParentKe Hua (father) Ke Lingling[a] (born 1951; Chinese: 柯玲玲; pinyin: kē líng líng; also known as Ke Xiaoming (柯小明, kē xiǎo míng)) is the ex-wife of Xi Jinping, the current General Secretary of the Chinese Communist Party (also known as the paramount leader). She is from Puning, Guangdon...

约翰斯顿环礁

此條目可参照英語維基百科相應條目来扩充。 (2021年5月6日)若您熟悉来源语言和主题，请协助参考外语维基百科扩充条目。请勿直接提交机械翻译，也不要翻译不可靠、低品质内容。依版权协议，译文需在编辑摘要注明来源，或于讨论页顶部标记{{Translated page}}标签。约翰斯顿环礁Kalama Atoll 美國本土外小島嶼 Johnston Atoll 旗幟颂歌：《星條旗》The Star-Spangled Banner約翰斯頓環礁�...

Angelo

Disambiguazione – Se stai cercando altri significati, vedi Angelo (disambigua). L'Arcangelo Michele indossa un mantello e una corazza militare romana in questa rappresentazione del XVII secolo di Guido Reni, il celebre San Michele arcangelo caccia Lucifero, a Roma, Chiesa di Santa Maria Immacolata a Via Veneto. Un angelo, in alcune tradizioni religiose, è un essere spirituale che assiste e serve Dio o è al servizio dell'uomo lungo il percorso del suo progresso spirituale e della sua esis...

Celebrity Big Brother (British TV series) series 9

CBB9 redirects here. For the Canadian airport, see Osoyoos Airport. Season of television series Celebrity Big BrotherSeries 9Series nine logoPresented byBrian DowlingNo. of days23No. of housemates12WinnerDenise WelchRunner-upFrankie CocozzaCompanion showsBig Brother's Bit On The Side No. of episodes25ReleaseOriginal networkChannel 5Original release5 January (2012-01-05) –27 January 2012 (2012-01-27)Series chronology← PreviousSeries 8Next →Series 10 Celebrity Big...

Lambang Bulgaria

Lambang Bulgaria Lambang Bulgaria (Bulgaria: Герб на България [ˈɡɛrp nɐ bɐɫˈɡarijɐ]) terdiri dari perisai merah bergambar singa emas berdiri; dengan mahkota Kerajaan Bulgaria di atasnya. Perisai ditopang oleh dua singa emas dengan mahkota; di bawah perisai terdapat ranting daun ek dengan pita putih bertuliskan semboyan Persatuan Ciptakan Kekuatan. Deskripsi Lambang Bulgaria saat ini diadopsi pada tahun 1997. Lambang saat ini adalah versi lambang Bulgaria yang sedikit di...

حضارة

لمعانٍ أخرى، طالع حضارة (توضيح). وسط مدينة نيويورك أحد أبرز معالم الحضارة الحديثة أهرامات الجيزة أحد أهم معالم حضارة مصر القديمة. استمع إلى هذه المقالة (8 دقائق)noicon هذا الملف الصوتي أُنشئ من نسخة هذه المقالة المؤرخة في 29 مايو 2013 (2013-05-29)، ولا يعكس التغييرات التي ...

Stenoderus

Stenoderus Klasifikasi ilmiah Kerajaan: Animalia Filum: Arthropoda Kelas: Insecta Ordo: Coleoptera Famili: Cerambycidae Genus: Stenoderus Stenoderus adalah genus kumbang tanduk panjang yang tergolong famili Cerambycidae. Genus ini juga merupakan bagian dari ordo Coleoptera, kelas Insecta, filum Arthropoda, dan kingdom Animalia. Larva kumbang dalam genus ini biasanya mengebor ke dalam kayu dan dapat menyebabkan kerusakan pada batang kayu hidup atau kayu yang telah ditebang. Referensi TITAN: C...

Taw Phaya Gyi

PangeranGeorge Taw Phaya GyiNama asalတော်ဘုရားကြီးLahir(1922-05-06)6 Mei 1922Rangoon, Burma, British RajMeninggal9 April 1948(1948-04-09) (umur 25)Tatkon, Kotapraja Tatkon, Teritorial Bersatu Naypyidaw, BurmaSebab meninggalDibunuhKebangsaanBurmaAlmamaterUniversitas Rangoon (Sarjana)Dikenal atasMantan Pewaris Takhta BurmaSuami/istriKhin Kyi (m. 1945)AnakSoe Win Myo NaingOrang tuaKo Ko Naing Myat Phaya GalayKerabat Thibaw ...

2023 Belgorod Oblast incursions

Incident on the Russia-Ukraine border 2023 Belgorod Oblast incursionsPart of the attacks in western Russia during the Russian invasion of UkraineReported extent of territorial control during the raidsDateFirst raid: 22–23 May 2023(1 day)Second raid: 1–15 June 2023(2 weeks)Sporadic incursions: 17 June–17 December 2023 (6 months)LocationGrayvoronsky and Shebekinsky districts, Belgorod Oblast, Russia50°29′N 35°40′E / 50.483°N 35.667°E / 50.483...

Dominio Sudalpino

Carta strutturale semplificata delle Alpi Il Dominio Sudalpino (detto anche Falda Sudalpina, oppure, più semplicemente, Sudalpino) è un preciso settore della catena alpina, delimitato da lineamenti geodinamici rilevanti a scala regionale, che si estende dal Canavese alle Alpi Dinaridi per una lunghezza di circa 700 km; la sua larghezza è variabile da meno di 50 a 150 km. Questo settore risulta compreso tra il lineamento insubrico a settentrione e l'avampaese padano a sud. È cost...

Kawasan Konservasi Perairan Daerah Kabupaten Sorong

Kawasan Konservasi Perairan Daerah Kabupaten Sorong (KKPD Kabupaten Sorong) merupakan salah satu kawasan konservasi perairan daerah di Papua Barat Daya, Indonesia. Nama lain KKPD Kabupaten Sorong adalah Kawasan Konservasi Perairan Jamursba Medi (KKP Jamursba Medi). Dasar hukum penetapannya adalah Surat Keputusan Bupati Sorong Nomor 522/303/2015. Surat keputusan ini diterbitkan pada tanggal 5 Oktober 2015. Luas kawasan KKPD Kabupaten Sorong adalah 322,508 Hektare. Dalam sistem koordinat geogra...

Lamadaya

Waterfall in Sanaag, SomalilandLamadayaلَمَدايَLamadaya water falls in SanaagLocation in the Horn of AfricaShow map of SomalilandLamadaya (Africa)Show map of AfricaLocationCal Madow, Ogo Mountains, Sanaag, SomalilandCoordinates10°44′09″N 47°14′42″E / 10.73583°N 47.24500°E / 10.73583; 47.24500Elevation2,410 metres (7,907 ft)[1] Lamadaya (Somali: Lamadaaye, Arabic: لَمَدايَ, romanized: Lamādaya) are waterfalls that are...

Seibal

Archaeological site of the Maya civilization Structure A-3 at Seibal.[1] Stela 11 at Seibal. Seibal (Spanish pronunciation: [sejˈβal]), known as El Ceibal in Spanish, is a Classic Period archaeological site of the Maya civilization located in the northern Petén Department of Guatemala, about 100 km SW of Tikal. It was the largest city in the Pasión River region.[2] The site was occupied from the Preclassic Period through to the Terminal Classic, with a signifi...

Dalton Castle

Dalton CastleCastle pada tahun 2015Nama lahirBrett GiehlLahir04 Maret 1986 (umur 38)Rochester, New York, Amerika Serikat[1]Karier gulat profesionalNama ringAshley Remington[2]Brett Giehl[3]Dalton Caroline Castle[4]Dalton Castle[5]Tinggi5 ft 11 in (180 cm)[6]Berat217 pon (98 kg)[7]Asal dariCatalina Island (di ROH)[6]The Open Waters (di Chikara)[2]Debut2009[5] Brett Giehl[8][...

Foundations of mathematics

Basic framework of mathematics For the book by Hilbert and Bernays, see Grundlagen der Mathematik. Part of a series onMathematics History Index Areas Number theory Geometry Algebra Calculus and Analysis Discrete mathematics Logic and Set theory Probability Statistics and Decision theory Relationship with sciences Physics Chemistry Geosciences Computation Biology Linguistics Economics Philosophy Education Mathematics Portalvte This article needs additional citations for verification. Please he...

ERA-45

See also

References

Read other articles: