Androgen Receptor Modulator

Estromustine (EoM) is the active metabolite of Estramustine phosphate (HY-13627A). Estromustine binds to mutant androgen receptor (m-AR) with EC₅₀ of 2.6 μM in LNCaP, exhibits cytotoxicity in human prostate cells LNCaP with IC₅₀ of 9.73 μM.

ChEMBL22003 is a potential phase separation modulator of ARV7 that can bind to the ARV7 binding sites. ChEMBL22003 has potential for use in the research of prostate cancer.

2,2,5,7,8-Pentamethyl-6-Chromanol (Standard) is the analytical standard of 2,2,5,7,8-Pentamethyl-6-Chromanol. This product is intended for research and analytical applications. 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[1].

S-40503 is a tissue-selective androgen receptor (AR) agonist with a K_i of 14.9 nM for rat AR. S-40503 binds to AR with high specificity, exerts full agonistic effects in bone and muscle, acts as a partial agonist in the prostate, and preferentially targets anabolic tissues rather than androgen-dependent tissues. S-40503 can be used in the research of osteoporosis.

Androgen receptor modulator 3 is a selective modulator for androgen receptor that can be used for research of sarcopenia.

MK-4541 is an orally active and selective androgen receptor (AR) modulator. MK-4541 acts as an antagonist to inhibit 5α-reductase. MK-4541 inhibits proliferation and induces apoptosis in AR positive prostate cancer cells. MK-4541 significantly inhibited the growth of R3327-G prostate tumors in xenograft mouse model.

Acetyl-ACTH (3-24) (human, bovine, rat) is a fragment of proopiomelanocortin (POMC) peptide. POMC peptides such as adrenocorticotrophin (ACTH), which is the precursor of α-MSH, is also an agonist at the MC-1 receptor.

MK-3984 is a selective androgen receptor modulator (SARM). MK-3984 can be used for the research of muscle wasting associated with cancer.

(+)-JNJ-37654032 is an orally active and selective androgen receptor modulator. (+)-JNJ-37654032 can be used in the study of muscle-wasting diseases.

NEP28 is a selective androgen receptor modulator with an EC₅₀ of 2.90 nM in 22RV1 cells. NEP28 increases the activity of Aβ-degrading enzyme neprilysin. NEP28 is efficacious in muscle and brain without serious side effects on prostate in rats. NEP28 can be used for osteoporosis, sarcopenia, and Alzheimer's disease research.

LH-RH II (chicken) is one of the two forms of luteinizing hormone-releasing hormone (LHRH) the hypothalamus of the domestic hen, which are structural variants of mammalian LHRH. LH-RH II (chicken) enhances gonadotrophin release in the domestic chicken.

LG-121071 is an orally active and selective androgen receptor modulator with a K_i of 17 nM.

Acetyl-ACTH (4-24) (human, bovine, rat) is a fragment of proopiomelanocortin (POMC) peptide. POMC peptides such as adrenocorticotrophin (ACTH), which is the precursor of α-MSH, is also an agonist at the MC-1 receptor.

MeSeI exhibits a weak inhibitory activity against monoamine oxidase MAO-A and MAO-B (IC₅₀=198.8 µM). MeSeI regulates dopamine receptor D2 and norepinephrine receptor α2, β1, and exhibits antidepressant-like effect in mice. MeSeI is orally active.

LGD-2941 is an orally active, potent and selective androgen receptor modulator. LGD-2941 shows excellent anabolic activity in muscle with reduced effect on the prostate in a rat model of hypogonadism. LGD-2941 also improves bone strength in a rat model of post-menopausal osteoporosis.

FL442 is an Androgen Receptor (AR) modulator. FL442 exhibits strong inhibitory effects in AR-dependent prostate cancer cells, showing similar inhibitory efficiency to traditional antiandrogen drugs Bicalutamide (HY-14249) and Enzalutamide (HY-70002), while maintaining antiandrogenic activity against the AR mutant F876L, which is highly resistant to Enzalutamide. Pharmacokinetic studies of FL442 in mice reveal a long half-life (8 hours), good targeting (prostate tissue), and metabolic stability, and it effectively inhibits LNCaP tumor growth at low plasma concentrations (30 ng/mL).

Octinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo.

LGD-2226 (Standard) is the analytical standard of LGD-2226 (HY-105318). This product is intended for research and analytical applications. LGD-2226 is a selective and orally active androgen receptor modulator with an EC₅₀ of 0.2 nM and a K_i of 1.5 nM for human androgen receptor. LGD-2226 shows tissue selectivity in animal models, with reduced effects on prostate compared to muscle. LGD-2226 can be used for muscle wasting, osteoporosis and sexual dysfunction.

LGD-3303 (Standard) is the analytical standard of LGD-3303 (HY-103576). This product is intended for research and analytical applications. LGD-3303 is a selective androgen receptor modulator (SARM).