The nuclear receptor known as the androgen receptor (AR) is activated when either the androgenic hormones testosterone or dihydrotestosterone bind to it in the cytoplasm before moving into the nucleus. The receptor separates from supporting proteins after binding the hormone ligand, moves into the nucleus, dimerizes, and then activates transcription of androgen-responsive genes. The progesterone receptor is most similar to the androgen receptor, and progestins can block the androgen receptor when used in higher doses. The androgen receptor's primary role is that of a DNA-binding transcription factor that controls gene expression. The development and maintenance of the male sexual phenotype depend heavily on genes that are regulated by androgen. Complete androgen insensitivity (CAIS) is a condition that is also correlated with mutations in this gene.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V60130 | Luxdegalutamide (ARV766) | 2750830-09-0 | Luxdegalutamide (ARV-766) is a potent oral protein degrading chimeric (PROTAC) protein degrader. |
|
V4852 | LY-2452473 | 1029692-15-6 | LY2452473 is a novel, potent, selective and orally bioavailable androgen receptor modulator (SARM) with potential tissue-selective androgenic/anti-androgenic activity. |
|
V1769 | Megestrol Acetate (BDH1298) | 595-33-5 | Megestrol acetate (formerly BDH1298, SC10363; BDH-1298; SC-10363; Megace; Ovaban; Pallace; Maygace; Megestil; Niagestin)is a synthetic progestogen derivative that has been approved for use in the treatment of breast cancer and loss of appetite. |
|
V4324 | MK-0773 | 606101-58-0 | MK-0773 (PF-05314882) is a novel and potent SARM (selective androgen receptor modulator) that binds to AR with an IC50 of 6.6 nM and with the potential for the prevention and treatment of muscle wasting associated with cancer. |
|
V1759 | MK-2866 (GTx-024) | 841205-47-8 | Ostarine (aslo known as Enobosarm, GTx024, MK2866, GTx-024, MK-2866) is a novel, potent and selective androgen receptor modulator (SARM) with potential antitumor activity. |
|
V40329 | N-Desmethyl Apalutamide | 1332391-11-3 | N-Desmethyl Apalutamide is the CYP2C8 and CYP3A4-mediated, N-demethylated and active metabolite of Apalutamide, but the potency is less than the parent drug. |
|
V33450 | N-desmethyl Enzalutamide (N-desmethyl MDV 3100) | 1242137-16-1 | N-desmethyl Enzalutamide (N-desmethyl MDV 3100) is an active metabolite of Enzalutamide which is is a novel, potent, orally bioavailable, organic, non-steroidal small molecule, second-generation androgen-receptor (AR) antagonist. |
|
V3988 | ORM-15341 | 1297537-33-7 | ORM-15341 is a novel, potent and full antagonist of human androgen receptor (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. |
|
V7564 | Proxalutamide | 1398046-21-3 | Proxalutamide (GT0918;GT-0918) is a novel, oral and potent androgen receptor/AR antagonist or nonsteroidal antiandrogen (NSAA). |
|
V83204 | Rad-150 | 1208070-53-4 | RAD150, esterized form of RAD-140, is a nonsteroidal androgen receptor modulator (IC50 = 130 nM). |
|
V14099 | RU-58841 | 154992-24-2 | RU-58841 is a new specific a candidate of choice for the treatment of acne, androgenetic alopecia and hirsutism. |
|
V14195 | S-23 | 1010396-29-8 | S-23 is an oral selective androgen receptor modulator (SARM) with Ki of 1.7 nM. |
|
V1770 | Spironolactone (SC9420) | 52-01-7 | Spironolactone(SC9420; SC-9420; SC 9420; Spiresis; Spiridon) is a potent androgen receptor/AR antagonist with potential antineoplastic activity. |
|
V4069 | Testolone (RAD140) | 1182367-47-0 | Testolone (formerly known as RAD140) is a novel, potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM) that is being investigated for the treatment of conditions such as muscle wasting and breast cancer. |
|
V3368 | TRC253 | 2110428-64-1 | JNJ-63576253 (TRC-253) is a potent and orally bioactive androgen receptor complete antagonist, with IC50s of 37 and 37 for F877L mutant AR and wild-type AR in LNCaP cells, respectively. |
|
V3752 | UT-155 | 2031161-35-8 | UT-155 is a potent and selective androgen receptor (AR) degrader (SARD) that markedly reduces the activity of wild-type and splice variant isoforms of AR at submicromolar doses. |
|
V38848 | UT-34 | 2168525-92-4 | UT-34 (UT34) is a novel, selective, and orally bioavailable pan-androgen receptor (AR) antagonist and also aselective androgen receptor degrader (SARD)with anti-prostate cancer activity. |
|
V50982 | WAY-324106 | 1351506-85-8 | androgen receptor modulator |
|
V50997 | WAY-324109 | 1351360-79-6 | androgen receptor modulator |
|
V51003 | WAY-621998 | 743475-40-3 | androgen Receptor modulator |
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