Female Reproductive System Disease

Giredestrant (GDC-9545) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC₅₀ of 0.03 nM. Giredestrant promotes the degradation of ERα protein, including the ESR1^Y537S mutant ERα. Giredestrant reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant induces tumor regression in both ESR1^Y537S mutant and wild-type ERα tumor models. Giredestrant can be used for the research of ER⁺ breast cancer.

Cetrorelix (SB-75) is a competitive gonadotropin-releasing hormone receptor (GnRHR) antagonist with a K_d of 0.19 nM. Cetrorelix inhibits the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), thereby suppressing the secretion of downstream sex steroids. Cetrorelix prevents ovulation, induces reversible reproductive shutdown and azoospermia, reduces ovarian fibrosis, improves superovulation outcomes, and inhibits chemotherapy-induced mitochondria-dependent apoptosis. Cetrorelix is applicable for fertility assistance research.

Cetrorelix (SB-75) acetate is a competitive gonadotropin-releasing hormone receptor (GnRHR) antagonist with a K_d of 0.19 nM. Cetrorelix acetate inhibits the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), thereby suppressing the secretion of downstream sex steroids. Cetrorelix acetate prevents ovulation, induces reversible reproductive shutdown and azoospermia, reduces ovarian fibrosis, improves superovulation outcomes, and inhibits chemotherapy-induced mitochondria-dependent apoptosis. Cetrorelix acetate is applicable for fertility assistance research.

Ternidazole hydrochloride is a nitroimidazole Antibiotic with anti-pathogenic microbial activity. Ternidazole hydrochloride kills and inhibits the visible growth of Clostridium perfringens type A in vitro. Ternidazole hydrochloride helps improve the therapeutic efficacy against bacterial vaginosis, candidal vaginitis and mixed vaginitis. Ternidazole hydrochloride effectively alleviates chronic alcoholism. Ternidazole hydrochloride can be used in research related to vaginitis, pathogenic microbial infections and chronic alcoholism.

LysoPC (18:3) is a type of lysophospholipid metabolite with biomarker properties. LysoPC (18:3) stably exists in human follicular fluid, and its abundance dynamically changes with age, synchronously regulating the body's lipid metabolism process, follicular development process and oocyte maturation process. The down-regulation of LysoPC (18:3) content is associated with breast cancer lesions and follicular aging changes accompanied by in vitro fertilization in elderly women. LysoPC (18:3) can be used in studies related to breast cancer and infertility in elderly women.

ML345 is a potent and selective inhibitor of insulin-degrading enzyme (IDE) and NLRP3, with an IC₅₀ of 188 nM against IDE. ML345 targets the Cys819 residue of IDE to inhibit IDE. ML345 selectively binds to NLRP3 in a non-covalent manner. ML345 inhibits inflammatory cytokines (IL-1β, IL-6) and exhibits potent anti-inflammatory activity. ML345 exerts a protective effect against miscarriage.

Meptyldinocap (2,4-DNOPC) is a fungicide and cytotoxic agent that acts against powdery mildew. Meptyldinocap upregulates the phosphorylation levels of ERK1/2, JNK and p38. Meptyldinocap induces apoptosis and endoplasmic reticulum stress, disrupts calcium homeostasis, inhibits cell proliferation and migration, downregulates the expression of proliferation- and pregnancy-related genes, and triggers mitochondrial dysfunction. Meptyldinocap can be used in studies related to powdery mildew and implantation failure.

MS152 is an orally active, blood-brain barrier penetrant inhibitor of EHMT2/G9a and EHMT1/GLP, with IC₅₀s of 76 nM and 126 nM, repsectively. MS152 reduces H3K9me2 levels and reactivates maternally silenced Prader-Willi syndrome (PWS) genes. MS152 significantly improves perinatal lethality and growth retardation in mouse models, and is applicable to research related to Prader-Willi syndrome.

1-Cyclohexanol (Hydroxycyclohexane; NSC 5471) is an orally active Cramer Class I flavor ingredient that can be used in fragrances. 1-Cyclohexanol has a wide margin of safety and is environmentally friendly.

Dienestrol is an orally active nonsteroidal estrogen. Dienestrol prevents the formation of implantation swellings in the uterus by inhibiting ovum discharge.

Prothioconazole is an orally active broad-spectrum fungicide. Prothioconazole weakly inhibits CaCYP51 activity in Candida albicans, with an apparent IC₅₀ of approximately 120 μM. Prothioconazole disrupts Microtubule stability by reducing the acetylation level of α-tubulin. Prothioconazole induces Mitochondrial dysfunction, oxidative stress, DNA damage, and Apoptosis. Prothioconazole accumulates ¹⁴-methylated sterols and depletes ergosterol in cells, culture media, plants, and animals. Prothioconazole interferes with pyruvate metabolism and glycolysis/gluconeogenesis processes in mouse liver, downregulates Fasn mRNA expression, and induces hepatotoxicity and renal metabolic disorders. Prothioconazole reduces the fertility of female mice. Prothioconazole inhibits body weight gain and increases liver/kidney indices in mice. Prothioconazole can be used in studies related to candidiasis.

DIM-3,5-Cl2 is an inverse NR4A1/NR4A2 agonist with K_D values of 7.7 μM and 12.0 μM for NR4A1 and NR4A2, respectively. DIM-3,5-Cl2 acts as an inverse agonist to downregulate pro-oncogenic and proendometriotic gene products, and as an agonist to enhance NR4A1/2/Sp1/Sp4-mediated CD71 transactivation. DIM-3,5-Cl2 induces ferroptosis via ROS formation, lipoperoxidation, MDA production, and reduced GPX4, SLC7A11 expression. DIM-3,5-Cl2 induces apoptosis via PARP and caspase-3 cleavage, reduced BCL-2 expression, and inhibits cancer cell viability. DIM-3,5-Cl2 can be used for the research of triple negative breast cancer, endometriosis, and colorectal cancer.

Ternidazole is a nitroimidazole Antibiotic with anti-pathogenic microbial activity. Ternidazole kills and inhibits the visible growth of Clostridium perfringens type A in vitro. Ternidazole helps improve the therapeutic efficacy against bacterial vaginosis, candidal vaginitis and mixed vaginitis. Ternidazole effectively alleviates chronic alcoholism. Ternidazole can be used in research related to vaginitis, pathogenic microbial infections and chronic alcoholism.

4,8-Dioxa-3H-perfluorononanoic acid is an ether-substituted polyfluoroalkyl compound and also a ligand of human pregnane X receptor (hPXR), which binds to the ligand-binding domain of hPXR. 4,8-Dioxa-3H-perfluorononanoic acid targets Arg-410, Lys-210, Lys-226, Met-323 and His-327 residues. Its binding process relies on long-range electrostatic interactions, and no significant hydrogen bonds form with hPXR residues. 4,8-Dioxa-3H-perfluorononanoic acid is used as a substitute for PFOA in Germany. 4,8-Dioxa-3H-perfluorononanoic acid is detectable in environmental matrices such as river water near fluoride production plants, accumulates in organisms including grass, deer liver and locusts, and is present in plasma samples of populations in southern Germany.

hFSH-β-(33-53) is a polypeptide corresponding to residues 33-53 of hFSH-β, and also a follicle-stimulating hormone (FSH) antagonist. hFSH-β-(33-53) stimulates basal estradiol synthesis in cells. hFSH-β-(33-53) prolongs vaginal estrus in mice with normal estrous cycles.

BAY-1128688 is a selective, orally active aldo-keto reductase family 1 member C3 (AKR1C3) inhibitor with an IC₅₀ of 1.4 nM. BAY-1128688 inhibits OATP, BSEP, MRP4, NTCP, UGT1A1, MRP2, and MRP3. BAY-1128688 induces reactive oxygen species (ROS) production, inhibits the mitochondrial electron transport chain, and increases circulating androsterone, etiocholanolone, dihydrotestosterone, and serum bilirubin concentrations. BAY-1128688 alters bilirubin disposition, leading to elevated plasma bilirubin, independent of liver injury. BAY-1128688 can be used in research on endometriosis and polycystic ovary syndrome.

Norgestomet is a synthetic 19-nortestosterone-derived progestin analog specifically used for estrus synchronization and reproductive regulation in cattle. Norgestomet reduces the incidence of short luteal phases in postpartum lactating beef cattle, enhances luteal function, and increases the pregnancy rate of timed breeding. Norgestomet suppresses estrus during embryo implantation, synchronizes the timing of estrus resumption, and improves the calving rate of first timed artificial insemination in pubertal beef heifers.

P2X4 antagonist-1 is a P2X4 receptor antagonist with an IC₅₀ of 15 nM. P2X4 antagonist-1 inhibits ATP (HY-B2176)-induced calcium influx. P2X4 antagonist-1 can be used for the research of pain syndromes, endometriosis, cancer.

1-Cyclohexanol₁₁ (Hydroxycyclohexane₁₁; NSC 54711₁₁) is the deuterium labeled 1-Cyclohexanol (HY-Y1217). 1-Cyclohexanol is an orally active Cramer Class I flavor ingredient that can be used in fragrances. 1-Cyclohexanol has a wide margin of safety and is environmentally friendly.

Giredestrant tartrate (GDC-9545 tartrate) is an orally active, full, selective Estrogen receptor α (ERα) degrader and antagonist with a DC₅₀ of 0.03 nM. Giredestrant tartrate promotes the degradation of ERα protein, including the ESR1^Y537S mutant ERα. Giredestrant tartrate reduces uterine wet weight in immature rats and induces a low cuboidal phenotype in their endometrial epithelium. Giredestrant tartrate induces tumor regression in both ESR1^Y537S mutant and wild-type ERα tumor models. Giredestrant tartrate can be used for the research of ER⁺ breast cancer.