Androgen Receptors

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Product Name
Application
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Product Citation
  1. Androgen Receptor antagonist

    (R)-Bicalutamide is an active competitive non-steroidal androgen receptor antagonist with an IC50 of 0.17 μM for MDA 453 cells.
  2. Androgen antagonist

    17 alpha-propionate is a new topical and peripherally selective androgen antagonist.
  3. Androgen Receptor agonist

    Andarine (GTX-007) is an investigational selective androgen receptor modulator (SARM).
  4. Androgen Receptor antagonist

    Bicalutamide is an oral non-steroidal anti-androgen used in the treatment of prostate cancer and hirsutism.
  5. Androgen Receptor Modulators

    Ostarine is an androgen receptor modulator (SARM)
  6. Androgen receptor antagonist

    Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.
  7. Androgen receptor antagonist

    MDV3100 is androgen-receptor inhibitor. Highly recommended inhibitor in AR research.
  8. Megestrol Acetate is a progesterone derivative with antineoplastic properties
  9. CYP17 inhibitor

    TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor.
  10. ASC-J9 suppresses castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors.
  11. Androgen Receptor antagonist

    Cyproterone acetate is a synthetic derivative of 17-hydroxyprogesterone, and acts as an androgen receptor antagonist as well as a weak progesterone receptor agonist with weak progestational and glucocorticoid activity.
  12. AR antagonist

    RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.
  13. human AR (hAR) antagonist

    ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct.
  14. AR inhibitor downregulator

    AZD-3514 is a potent androgen receptor downregulator with potential anticancer cancer activity.
  15. androgen receptor modulator

    GSK-2881078 is a selective androgen receptor modulator (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting to improve their physical function.
  16. Androgen receptor (AR) modulator

    BMS-564929 is a novel, highly potent, orally active, nonsteroidal tissue selective androgen receptor (AR) modulator, and this compound has been advanced to clinical trials for the treatment of age-related functional decline.
  17. Bopindolol malonate is a non-selective, potent, long-acting beta adrenoceptor antagonist. It demonstrates inhibition of H2O2-induced lipid peroxdiation.
  18. CYP17A1/androgen synthesis inhibitor

    Orteronel (TAK700) is an androgen synthesis inhibitor. It selectively inhibits the enzyme CYP17A which is expressed in testicular, adrenal, and prostatic tumor tissues.
  19. androgen-receptor (AR) antagonist

    N-desMethyl EnzalutaMide is used in the treatment of disorders involving androgen, estrogen and progesterone receptors.
  20. androgen receptor modulator

    LGD-4033 is an investigational selective androgen receptor modulator for treatment of conditions such as muscle wasting and osteoporosis, currently under development by Ligand Pharmaceuticals.
  21. Androgen receptor modulator

    MK-0773, one of selective androgen receptor modulators (SARMs), is a 4-aza-steroid that exhibited tissue selectivity in humans (IC50= 6.6 nM).
  22. Androgen receptor antagonist

    ODM-201 is a potent and full antagonists for human AR (hAR) with IC50 values of 26 nM by transactivation assays in AR-HEK293 cells.
  23. Androgen Receptor antagonist

    EPI-001 is an antagonist of the androgen receptor (AR) that acts by binding covalently to the N-terminal domain (NTD) of the AR and blocking protein-protein interactions required for transcriptional activity of the AR and its splice variants (IC50 for inhibition of AR NTD transactivation ?? 6 μM)
  24. MI-136 inhibits DHT-induced expression of androgen receptor (AR) target genes.
  25. androgen receptor modulator (SARM)

    LY2452473 is an orally bioavailable selective androgen receptor modulator (SARM), with potential tissue-selective androgenic/anti-androgenic activity.
  26. Androsterone is a steroid hormone produced in the body from 5α-reduced metabolites of dehydroepiandrosterone. It is the major androgen excreted in urine as a metabolite of testosterone and is used as the international reference standard for androgenic activity.
  27. Androgen receptor antagonist

    Spironolactone is a potent antagonist of the androgen receptor.
  28. OC2 inhibitor

    CSRM617 Hydrochloride is an inhibitor of the transcription factor ONECUT2 (OC2), thereby suppressing metastasis in mice.
  29. Androgen metabolite

    Beta-Cortol is an androgen metabolite present in adults.
  30. 2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the anti-oxidant moiety of vitamin E (α-tocopherol). 2,2,5,7,8-Pentamethyl-6-Chromanol has potent androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines.
  31. AR antagonist

    Proxalutamide (GT0918) is a potent androgen receptor (AR) antagonist.
  32. androgen ligand

    Androstanolone acetate is an androgen ligand, which targets androgen receptor (AR). Androstanolone acetate binds to cIAP1 ligand Bestatin via a linker to form PROTACs.
  33. androgen receptor modulator

    ACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively.
  34. CB1 agonist

    Leelamine hydrochloride is a tricyclic diterpene molecule that is extracted from the bark of pine trees. Leelamine hydrochloride is a cannabinoid receptor type 1 (CB1) agonist and a inhibitor of SREBP1-regulated fatty acid/lipid synthesis in prostate cancer cells that is not affected by androgen receptor status.
  35. androgen receptor antagonist

    D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
  36. androgen receptor/CYP17A1 dual inhibitor

    ODM-204 is novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme, with IC50s of 80?nM and 22 nM, respectively.
  37. Androgen receptor partial agonist

    YK11 is a partial agonist of androgen receptor, with osteogenic activity.
  38. AR antagonist

    UT-155 is a selective and potent androgen receptor (AR) antagonist, with a Ki of 267 nM for UT-155 binding to AR-LBD.
  39. Topilutamide is a topical nonsteroidal antiandrogen (NSAA).
  40. androgen receptor modulator

    GLPG0492 is a novel selective androgen receptor modulator; exhibited anabolic activity on muscle, strongly dissociated from the androgenic activity on prostate after oral dosing.
  41. Androgen receptor antagonist

    Nilutamide (Nilandron) is a non-steroidal anti-androgen drug proposed in the treatment of metastatic prostatic carcinoma.
  42. androgen receptor modulator

    RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM).
  43. SARD ligand

    (R)-UT-155 (compound 11) is a selective androgen receptor degrader (SARD) ligand. Less active than the S-isomer.
  44. selective androgen receptor modulator

    S-23 is an orally active selective androgen receptor modulator (SARM) with a Ki of 1.7 nM.
  45. androgen receptor modulator

    AC-262536 is a selective androgen receptor (SAR) molecule. It has partial agonist activity with respect to testosterone and suppresses luteinizing hormone.
  46. Antiandrogenic agent

    4'-Methoxyresveratrol (4'-O-Methylresveratrol) is a polyphenol derived from Dipterocarpaceae, with antiandrogenic, antifungal and anti-inflammatory activities.
  47. Androgen receptor antagonist

    TRC253, also known as JNJ63576253, is a potent and orally active androgen receptor antagonist.

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