Male Reproductive System Disease

Phentolamine is an orally active, selective α1 and α2 Adrenergic receptor antagonist. Phentolamine antagonizes the vasodilatory effect of Cromakalim (HY-110011) on isolated circumflex coronary artery segments in dogs. Phentolamine reduces systemic vascular resistance and increases cardiac output. Phentolamine improves erectile dysfunction. Phentolamine can be used for the research of erectile dysfunction.

Melanotan (MT)-II is a melanocortin receptor agonist. Melanotan (MT)-II activates melanocortin receptor 3 and melanocortin receptor 4, and stimulates the release of central endogenous oxytocin. Melanotan (MT)-II reverses recognition memory impairment, increased anxiety levels and reduced exploratory tendency in zebrafish exposed to short-term high-fat diet. Melanotan (MT)-II improves impaired social behavior indicators in mouse models of autism spectrum disorder. Melanotan (MT)-II induces weight loss, reduces food intake and exerts anorectic effects. Melanotan (MT)-II increases intracavernous pressure and erectile activity in brown rats. Melanotan (MT)-II can be used in studies related to memory impairment, anxiety, reduced exploratory behavior, autism spectrum disorder, obesity and erectile dysfunction.

6:2 Cl-PFAES is an orally effective alternative to Perfluorooctane sulfonate. 6:2 Cl-PFAES significantly inhibits the growth of zebrafish and induces reproductive toxicity. 6:2 Cl-PFAES reduces the relative weights of epididymis and testis in male BALB/c mice. 6:2 Cl-PFAES can be used in the chrome plating industry.

Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC₅₀ of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC₅₀s of 180 nM, and 11 nM, while IC₅₀s are >1000 nM for PDE3 and PDE4. Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes^[1]-[6].

Glycylglycine is a non-selective glycylglycine dipeptidase substrate and iNOS inhibitor. Glycylglycine can cross the cell membrane by passive diffusion and is hydrolyzed to glycine in the cell, participating in energy metabolism and antioxidant processes. Glycylglycine promotes spermatogonial stem cells (SSCs) proliferation, inhibits astrocyte overactivation and reduces nitric oxide (NO) release, while upregulating the expression of neurotrophic factors (such as PDGFA, FGF2, CNTF) to support nerve myelin repair. Glycylglycine can be used to study male reproductive biology (such as SSCs proliferation regulation) and neurodegenerative diseases (such as neuroprotective mechanisms in multiple sclerosis).

Monobutyl phthalate is an orally active metabolite of Di-n-butyl phthalate (HY-Y0304) and an embryotoxic agent. Monobutyl phthalate regulates mesodermal lineage gene expression, inhibits uterine decidualization, reduces fetal testosterone levels without directly binding to the androgen receptor, and induces teratogenic effects during organogenesis. Monobutyl phthalate induces testicular oxidative stress and sperm abnormalities. Monobutyl phthalate can be used in studies of developmental toxicity and male reproductive toxicity.

Melamine is an orally active inducer of Apoptosis. Melamine induces animal disease models. Melamine affects the activity of Sertoli cell and can be used for research on male reproductive function. Melamine also has neurotoxicity and nephrotoxicity. Melamine induces cognitive impairment and acute kidney injury models. Melamine can also be used to induce bladder cancer and urinary stone models.

Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC₅₀ of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC₅₀s of 180 nM, and 11 nM, while IC₅₀s are >1000 nM for PDE3 and PDE4. Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes^[1]-[6].

Phentolamine hydrochloride is an orally active, selective α1 and α2 Adrenergic receptor antagonist. Phentolamine hydrochloride antagonizes the vasodilatory effect of Cromakalim (HY-110011) on isolated circumflex coronary artery segments in dogs. Phentolamine hydrochloride reduces systemic vascular resistance and increases cardiac output. Phentolamine hydrochloride improves erectile dysfunction. Phentolamine hydrochloride can be used for the research of erectile dysfunction.

Diethyl phthalate is an orally active plasticizer and detergent base. Diethyl phthalate increases the activities of ACP, ALP, SDH, and ALT in liver, muscle, or both tissues. Diethyl phthalate induces dose-dependent mortality and sluggish behavior in freshwater fish. Diethyl phthalate may induce male reproductive toxicity. Diethyl phthalate is added to plastic polymers to help maintain their flexibility.

DL-threo-PDMP hydrochloride is a competitive glucosylceramide synthase (GCS) inhibitor and antimalarial agent. DL-threo-PDMP hydrochloride competitively inhibits the activity of GCS. DL-threo-PDMP hydrochloride restores cisplatin sensitivity in cisplatin-resistant testicular germ cell tumor cells. DL-threo-PDMP hydrochloride blocks the growth of ring-stage Plasmodium falciparum parasites.

Methylliberine is an orally active adenosine A1 receptor modulator. Methylliberine inhibits spermatogenesis and induces testicular atrophy.

Dihexyl phthalate is an orally active phthalate ester (PAEs) widely used as a plasticizer, and it acts as an environmental endocrine disruptor. Dihexyl phthalate exhibits endocrine-disrupting and reproductive toxic properties, induces oxidative stress and inflammation, and ultimately causes apoptosis and damage to reproductive organs such as the testes. Dihexyl phthalate can be used in studies related to developmental toxicity, embryonic lethality, teratogenicity, and abnormal development of the male reproductive system.

Tripotassium hydroxycitrate is an orally active, multi-target, multi-bioactive organic acid. Tripotassium hydroxycitrate activates Nrf2 and its downstream molecule GPX4, increases glutathione levels, and thereby inhibits ferroptosis. Tripotassium hydroxycitrate activates the Nrf2/Keap1 and ACLY/NF-κB signaling pathways, upregulates the activities of antioxidant enzymes such as superoxide dismutase, reduces MDA content, thereby alleviating oxidative stress and renal tubular epithelial cell apoptosis, and improves pulmonary vascular and right ventricular remodeling. Tripotassium hydroxycitrate activates both the AMPK and mTORC1/S6K pathways, triggers the unfolded protein response, arrests the cancer cell cycle, and induces DNA fragmentation.

3',4'-Dihydroxyflavone is an orally active antioxidant. 3',4'-Dihydroxyflavone inhibits the NF-κB, JAK1/STAT1, AP-1, IRF3, and MAPK/MEK/ERK pathways, while activating Nrf2 and reducing Keap1, thereby exerting anti-inflammatory and antioxidant effects. 3',4'-Dihydroxyflavone inhibits NO, PGE₂, pro-inflammatory cytokines, and ROS production, upregulates GSH, and activates K_ATP channels, adenosine A₃ receptors, and GABA_A receptors. 3',4'-Dihydroxyflavone inhibits PPARγ expression and adipogenic differentiation, induces osteogenic differentiation; it also inhibits 5-lipoxygenase and xanthine oxidase, weakly inhibits PARP1, and scavenges DPPH and superoxide radicals. 3',4'-Dihydroxyflavone can be used for research on peripheral nerve injury, septic shock, obesity, influenza A virus infection, infertility, and diabetic complications.

DL-Methionine methylsulfonium chloride (DL-MMSC) is an orally effective methionine-derived sulfonium salt that promotes gastric emptying and gastrointestinal transit. DL-Methionine methylsulfonium chloride attenuates oxidative stress and inflammatory responses, and enhances anti-apoptotic (apoptosis) signaling, thereby ameliorating Sodium metabisulfite (HY-Y1326)-induced testicular dysfunction and semen quality impairment. DL-Methionine methylsulfonium chloride is applicable for research on functional dyspepsia, gastrointestinal motility, and male reproductive function injury.

Diethyl phthalate-d₄ is the d₄ labeled Diethyl phthalate (HY-Y0284). Diethyl phthalate is an orally active plasticizer and detergent base. Diethyl phthalate increases the activities of ACP, ALP, SDH, and ALT in liver, muscle, or both tissues. Diethyl phthalate induces dose-dependent mortality and sluggish behavior in freshwater fish. Diethyl phthalate may induce male reproductive toxicity. Diethyl phthalate is added to plastic polymers to help maintain their flexibility.

Mono-Cyclohexyl Phthalate-3,4,5,6-d₄ is the d₄-labeled Monocyclohexyl phthalate (HY-W701876). Monocyclohexyl phthalate is a phthalate metabolite and a competitive UGT1A9 inhibitor with an IC₅₀ of 3.29 μM and a K_i of 0.09 μM. Monocyclohexyl phthalate can be used in research on impaired sperm quality and birth weight.

Prostaglandin D1 (PGD1) is a CatSper activator that triggers Ca²⁺ influx through sperm-specific Ca²⁺ channels via the prostaglandin binding site and competes with other prostaglandins.

Perfluorotetradecanoic acid (PFTeDA) is an orally active perfluoroalkyl substance. Perfluorotetradecanoic acid directly binds to the ligand-binding domain of purified hPPARγ, with a K_d value of 157.8 μM. Perfluorotetradecanoic acid significantly reduces the activity of the SIRT1/PGC1α and AMPK signaling pathways while stimulating the activity of the AKT1/mTOR signaling pathway. Perfluorotetradecanoic acid significantly upregulates the expression of corticosterone biosynthesis genes. Perfluorotetradecanoic acid increases ROS levels and promotes Apoptosis. Perfluorotetradecanoic acid impairs Leydig cell function and male reproductive endocrine function in adult male rats.