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You are here:Home-Inhibitors & Agonists-Nuclear Receptor/Transcription Factor-Androgen Receptor (AR)

Request The Product List ofAndrogen Receptor (AR) Androgen Receptor (AR)

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)

Cat. No. Product Name CAS No. Information
GY03856

CB-03-01

19608-29-8

Cortexolone 17 alpha-propionate (CB-03-01, Clascoterone) is a topical and peripherally selective androgen antagonist, displays a strong local antiandrogenic activity in hamster's flank organ test, does not exhibit antiandrogenic activity after subcutaneous injection in vivo.

GY03855

RU58841

154992-24-2

A nonsteroidal, specific androgen receptor inhibitor; be useful for the topical treatment of androgen-dependent skin disorders such as acne, androgenetic alopecia and hirsutism.

GY10096

KCI807

6665-68-5

KCI807 (KCI-807) is a lead molecule that selectively disrupts ELK1-dependent promoter activation by wild-type and variant Ars (IC50=0.53 uM) without interfering with ELK1 activation by ERK; binds to AR (Kd=69.2 nM), blocking ELK1 binding, and selectively blocks recruitment of AR to chromatin by ELK1; primarily affects a subset of AR target growth genes selectively suppressing AR-dependent growth of PC cell lines with a better inhibitory profile than Enzalutamide; also inhibits in vivo growth of castration/enzalutamide-resistant cell line-derived and patient-derived tumor xenografts.

GY10282

IMTPPE

IMTPPE (SID 3712502) is a novel small molecule capable of inhibiting androgen receptor (AR) transcriptional activity (IC50=1 uM) and protein level in C4-2 prostate cancer cells; IMTPPE inhibited proliferation of AR-positive, but not AR-negative, prostate cancer cells in culture. IMTPPE inhibited the transcriptional activity of a mutant AR lacking the ligand-binding domain (LBD); IMTPPE inhibited the growth of 22Rv1 xenograft tumor, a model for enzalutamide-resistant prostate cancer.

GY10072

UT-34

2168525-92-4

UT-34 is a selective androgen receptor degrader (SARD) ligand.Orally Bioavailable Androgen Receptor Degrader, Potential Next-Generation Therapeutic for Enzalutamide-Resistant Prostate Cancer.

GY02293

N-desmethyl Enzalutamide

1242137-16-1

Amajor metabolite of Enzalutamide (MDV3100) which is an androgen-receptor (AR) antagonist for treatment of prostate cancer.

GY04046

LGD4033

1165910-22-4

A novel nonsteroidal, oral selective androgen receptor modulator (SARM), binds androgen receptor with high affinity (Ki=1 nM) and selectivity; has favorable pharmacokinetic profile, and increases lean body mass even during this short period without change in prostate-specific antigen.

GY03800

LGD-3033

917891-35-1

LGD-3303 is an orally available, brain-penetrant nonsteroidal selective androgen receptor modulator (SARM) that that shows little or no cross-reactivity with related nuclear receptors; has potent activity on levator ani muscle but is a partial agonist on the preputial gland and ventral prostate in a castrated rat model of androgen deficiency; enhances male-directed sexual preference, proceptive behavior, and lordosis behavior in sexually experienced, but not sexually naive, female rats.

GY01611

ODM-201

1297538-32-9

Darolutamide (ODM-201;BAY-1841788) is a potent wt/mutant androgen receptor (AR) inhibitor with Ki of 11 nM; inhibits wtAR/AR(F876L) with IC50 of 65/66 nM respectively, weak inhibition on AR(W741L) and AR(T877A); inhibits the nuclear translocation of AR and more efficaciously than enzalutamide or ARN-509 in VCaP cell line proliferation assay; reduces the growth of AR-overexpressing VCaP prostate cancer cells both in vitro and in a castration-resistant VCaP xenograft model.

GY01602

Andarine

401900-40-1

Andarine (S-4;GTx007) is a non-steroidal selective androgen receptor modulator (SARM) with Ki of 4 nM, efficaciously stimulated AR-mediated reporter gene expression; demonstrates in vivo androgenic and anabolic activity, stimulates the anabolic organs more than the androgenic organs; improves muscle strength and body composition and prevents bone loss in orchidectomized rats.

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