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Androgen Receptor

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Androgen Receptor Androgen receptor (AR) is a type of nuclear receptor that is activated by binding of either of the androgenic hormones testosterone or dihydrotestosterone in the cytoplasm and then translocating into the nucleus. Upon binding the hormone ligand, the receptor dissociates from accessory proteins, translocates into the nucleus, dimerizes, and then stimulates transcription of androgen responsive genes. The androgen receptor is most closely related to the progesterone receptor, and progestins in higher dosages can block the androgen receptor. The main function of the androgen receptor is as a DNA-binding transcription factor that regulates gene expression. Androgen regulated genes are critical for the development and maintenance of the male sexual phenotype. Mutations in this gene are also associated with complete androgen insensitivity (CAIS). www.MedChemExpress.com 1 Androgen Receptor Inhibitors, Agonists, Antagonists & Modulators (R)-UT-155 2,2,5,7,8-Pentamethyl-6-Chromanol Cat. No.: HY-112895A (PMC) Cat. No.: HY-111024 (R)-UT-155 (compound 11) is a selective androgen 2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the receptor degrader (SARD) ligand. Less active than anti-oxidant moiety of vitamin E (α-tocopherol). the S-isomer. 2,2,5,7,8-Pentamethyl-6-Chromanol has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Size: 250 mg, 500 mg Size: 10 mM × 1 mL, 100 mg 3,3'-Diindolylmethane ACP-105 (DIM; Arundine; HB 236) Cat. No.: HY-15758 Cat. No.: HY-112256 3,3'-Diindolylmethane is a strong, pure androgen ACP-105 is an orally available, selective amd receptor (AR) antagonist. potent androgen receptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively. Purity: 98.74% Purity: 98.37% Clinical Data: Phase 4 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 200 mg, 500 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Ailanthone Andarine (Δ13-Dehydrochaparrinone) Cat. No.: HY-N1943 (GTx-007; S-4) Cat. No.: HY-12023 Ailanthone (Δ13-Dehydrochaparrinone) is a potent Andarine (S-4) is an investigational selective inhibitor of both full-length androgen receptor androgen receptor modulator (SARM) and an active (AR) (IC50=69nM) and constitutively active partial agonist. truncated AR splice variants (AR1-651 IC50=309nM). Purity: 99.71% Purity: 99.51% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Androst-4-ene-3,17-diol, dipropanoate, (3β,17β)- Androstanolone acetate (Androst-4-ene-3β,17β-diol, dipropionate) Cat. No.: HY-U00272 Cat. No.: HY-111847 Androst-4-ene-3,17-diol, dipropanoate, (3β,17β)- Androstanolone acetate is an androgen ligand, is the dipropanoate of 4-Androstenediol, a which targets androgen receptor (AR). metabolite of testosterone. Androstanolone acetate binds to cIAP1 ligand Bestatin via a linker to form PROTACs. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 5 mg Apalutamide AZD3514 (ARN-509) Cat. No.: HY-16060 Cat. No.: HY-16079 Apalutamide (ARN-509) is a potent and competitive AZD3514 is a potent and oral androgen receptor androgen receptor (AR) antagonist, binding AR downregulator with Ki of 2.2 μM and has ability of with an IC50 of 16 nM. reducing AR protein expression. Purity: 99.69% Purity: 98.77% Clinical Data: Phase 3 Clinical Data: Phase 1 Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Bicalutamide Bifluranol Cat. No.: HY-14249 (BX341) Cat. No.: HY-U00229 Bicalutamide is a non-steroidal androgen Bifluranol (BX341) is an anti-androgen. receptor inhibitor. Purity: 99.61% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 200 mg, 500 mg, 1 g, 5 g Size: 1 mg, 5 mg, 10 mg, 20 mg BMS-564929 Boldenone Cypionate Cat. No.: HY-12111 Cat. No.: HY-118603 BMS-564929 is an androgen receptor (AR) agonist, Boldenone Cypionate is an androgenic anabolic binds to androgen receptor (AR) with a Ki of steroid. 2.11±0.16 nM. Purity: 98.70% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Boldenone Undecylenate Clascoterone (Cortexolone 17 alpha-propionate; Cortexolone (Ba 29038) Cat. No.: HY-17434 17α-propionate; CB-03-01) Cat. No.: HY-13331 Boldenone Undecylenate (Ba 29038) is a synthetic Clascoterone is a new topical and peripherally steroid which has a similar effect as the natural selective androgen antagonist. steroid testosterone; it is frequently used in veterinary medicine, though it is also used in humans. Purity: 96.33% Purity: 98.76% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Cyproterone acetate D4-abiraterone Cat. No.: HY-13604 (Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite) Cat. No.: HY-109619 Cyproterone acetate is an androgen receptor (AR) D4-abiraterone is a major metabolite of antagonist with IC50 of 7.1 nM, as well as a weak abiraterone. D4-abiraterone is an inhibitor of progesterone receptor agonist with weak CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) pro-gestational and glucocorticoid activity. and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor. Purity: 99.71% Purity: 99.42% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 250 mg, 500 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg Danazol Darolutamide Cat. No.: HY-B1029 (ODM-201; BAY-1841788) Cat. No.: HY-16985 Danazol is a derivative of the synthetic steroid Darolutamide (ODM-201;BAY-1841788) is a potent ethisterone, that suppresses the production of androgen receptor (AR) antagonist with an IC50 of gonadotrophins, and has some weak androgenic 26 nM in in vitro assay. effects. Purity: 99.91% Purity: 97.72% Clinical Data: Launched Clinical Data: Phase 3 Size: 10 mM × 1 mL, 100 mg, 250 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg www.MedChemExpress.com 3 Dehydroisoandrosterone 3-acetate DHEA (Prasterone; Dehydroisoandrosterone; (Dehydroepiandrosterone 3-acetate; DHEA acetate) Cat. No.: HY-B1405 Dehydroepiandrosterone) Cat. No.: HY-14650 Dehydroepiandrosterone 3-acetate is a DHEA (Prasterone) is one of the most abundant testosterone/estrogen precursor and known steroid hormones. DHEA (Prasterone) mediates its modulator of vertebrate aggression. action via multiple signaling pathways involving specific membrane receptors and via transformation into androgen and estrogen derivatives (e.g. Purity: >98.0% Purity: >98.0% Clinical Data: No Development Reported Clinical Data: Phase 4 Size: 10 mM × 1 mL, 1 g, 5 g Size: 10 mM × 1 mL, 100 mg, 500 mg Dimethylcurcumin DJ-V-159 (ASC-J9; GO-Y025) Cat. No.: HY-15194 Cat. No.: HY-114165 Dimethylcurcumin (ASC-J9) is an androgen DJ-V-159 is an agonist for G protein-coupled receptor degradation enhancer that effectively receptor family C group 6 member A (GPRC6A). suppresses castration resistant prostate cancer cell proliferation and invasion. Purity: 98.06% Purity: 99.99% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Enzalutamide Epiandrosterone (MDV3100) Cat. No.: HY-70002 (3β-Androsterone; trans-Androsterone; iso-Androsterone) Cat. No.: HY-I0352 Enzalutamide (MDV3100) is an androgen receptor Epiandrosterone is a steroid hormone with weak (AR) antagonist with an IC50 of 36 nM in LNCaP androgenic activity. Epiandrosterone is naturally prostate cells. produced by the enzyme 5α-reductase from the adrenal hormone DHEA. Purity: 99.71% Purity: >98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg Size: 10 mM × 1 mL, 1 g, 5 g Flutamide GLPG0492 (SCH 13521) Cat. No.: HY-B0022 Cat. No.: HY-18102 Flutamide is an antiandrogen drug, with its active GLPG0492 is a novel selective androgen receptor metablolite binding at androgen receptor with Ki modulator; exhibited anabolic activity on muscle, values of 55 nM, and primarily used to treat strongly dissociated from the androgenic activity prostate cancer. on prostate after oral dosing. Purity: 99.01% Purity: 99.66% Clinical Data: Launched Clinical Data: Phase 1 Size: 10 mM × 1 mL, 1 g, 5 g Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg GLPG0492 R enantiomer GSK-2881078 Cat. No.: HY-18102A Cat. No.: HY-100186 GLPG0492 R enantiomer is the R enantiomer of GSK 2881078 is a selective androgen receptor GLPG-0492, which is a novel selective androgen modulator potentially for the treatment of receptor modulator. cachexia. Purity: 99.51% Purity: 99.39% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg 4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Isosilybin B Leelamine hydrochloride Cat. No.: HY-N7045 Cat. No.: HY-110028 Isosilybin B, a flavonolignan isolated from Leelamine hydrochloride is a tricyclic diterpene silymarin, has anti-prostate cancer (PCA) activity molecule that is extracted from the bark of pine via inhibiting proliferation and inducing G1 phase trees.
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    Genera of l P l r a a n c r t u i c o e J Kalmanovich et al., J Gen Pract 2014, 2:3 Journal of General Practice DOI: 10.4172/2329-9126.1000153 ISSN: 2329-9126 Case Report Open Access Androgenic-Anabolic Steroid (Boldenone) Abuse as a Cause of Dilated Cardiomyopathy Eran Kalmanovich*, Sa'ar Minha, Marina Leitman, Zvi Vered and Alex Blatt Assaf Harofeh Medical Center, Aviv University, Israel *Corresponding author: Eran Kalmanovich, Department of Cardiology, Assaf Harofeh Medical Center, Zerifin, Sackler School of Medicine, Tel Aviv University, Israel, Tel: +972-50-5191121; E-mail: [email protected] Received date: Feb 27, 2014, Accepted date: Mar 27, 2014, Published date: Apr 3, 2014 Copyright: © 2014 Kalmanovich E, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. Case Presentation At admission 1-year follow up A 34-year old, previously healthy male, presented to the ER with EF% 20% 40% worsening dyspnea over a period of three weeks and the appearance of blood tinged sputum. Soon after presentation, the patient was LA diameter (mm) 3.9 3.8 hypoxemic and required mechanical ventilation. Chest X-ray LA area (cm2) 14.0 20 demonstrated bilateral infiltrates and he was admitted to the ICU with the tentative diagnosis of acute respiratory distress syndrome. LVEDD (cm) 6.1 5.6 Investigation by PICCO, Suggested the presence of heart failure were LVESD (cm) 5.1 3.3 and the patient was transferred to the ICCU.
  • WO 2018/190970 Al 18 October 2018 (18.10.2018) W !P O PCT

    WO 2018/190970 Al 18 October 2018 (18.10.2018) W !P O PCT

    (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2018/190970 Al 18 October 2018 (18.10.2018) W !P O PCT (51) International Patent Classification: GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, CI2Q 1/32 (2006.01) UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, (21) International Application Number: EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, PCT/US2018/021 109 MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, (22) International Filing Date: TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, 06 March 2018 (06.03.2018) KM, ML, MR, NE, SN, TD, TG). (25) Filing Language: English Declarations under Rule 4.17: (26) Publication Langi English — as to applicant's entitlement to apply for and be granted a patent (Rule 4.1 7(H)) (30) Priority Data: — as to the applicant's entitlement to claim the priority of the 62/484,141 11 April 2017 ( 11.04.2017) US earlier application (Rule 4.17(Hi)) (71) Applicant: REGENERON PHARMACEUTICALS, Published: INC. [US/US]; 777 Old Saw Mill River Road, Tarrytown, — with international search report (Art. 21(3)) New York 10591-6707 (US). — with sequence listing part of description (Rule 5.2(a)) (72) Inventors: STEVIS, Panayiotis; 777 Old Saw Mill Riv er Road, Tarrytown, New York 10591-6707 (US).