uterine

Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.

Tamoxifen Citrate is an orally active selective estrogen receptor modulator (SERM) that blocks estrogen activity in breast cells while activating estrogen signaling in cells such as those of the bone, liver, and uterus. As an Hsp90 activator, it enhances the ATPase activity of the Hsp90 chaperone complex, induces autophagy and apoptosis, and can be used to generate gene knockout models in CreER(T2) transgenic mice as well as liver injury models.

Ulipristal acetate (CDB-2914) is an orally bioavailable selective progesterone receptor modulator with anti-progesterone activity. It binds to the progesterone receptor (PR), inhibiting PR-mediated gene expression and interfering with progesterone activity in the reproductive system, potentially suppressing the growth of uterine leiomyomatosis. Additionally, ulipristal can be used as emergency contraception by inhibiting or delaying ovulation and affecting endometrial tissue.

Ulipristal is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure.

Carboprost (15(S)-15-Methyl Prostaglandin F2α) is a synthetic analogue of PGF2α with oxytocic properties, commonly used to restore uterine tone.

Estradiol (E2) is a naturally occurring steroidal sex hormone that is essential for female fertility and maintenance of secondary sexual characteristics. Estradiol upregulates IL-6 expression through estrogen receptor beta (ERβ).

Relugolix (RVT-601) is an orally available, non-peptide gonadotropin-releasing hormone (GnRH or luteinizing hormone-releasing hormone (LHRH)) antagonist, with potential antineoplastic activity. Relugolix competitively binds to and blocks the GnRH receptor in the anterior pituitary gland, which both prevents GnRH binding to the GnRH receptor and inhibits the secretion and release of both luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone from Leydig cells in the testes. Since testosterone is required to sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation.

Linzagolix is a small-molecule, non-peptide, orally active gonadotropin-releasing hormone antagonist (GnRH antagonist) which is under development by Kissei Pharmaceutical and ObsEva for the treatment of uterine fibroids, endometriosis, and adenomyosis. As of December 2020, it is under review for approval for uterine fibroids, is in phase III clinical trials for endometriosis, and is in phase II clinical studies for adenomyosis.

14-Deoxyandrographolide is a bioactive compound of Andrographis paniculata with hepatoprotective efficacy. It desensitizes hepatocytes to TNF-α-mediated apoptosis through the release of TNFRSF1A release.

Lauterine is a DNA topoisomerase inhibitor.

Nomegestrol (TX 066 free base) is an orally available, selective and potent full agonist of the progesterone receptor with potent anti-estrogenic, partial anti-androgenic and anti-gonadotropic activity.Nomegestrol is also a contraceptive progestin and is used in the study of endometriosis and meningiomas.

LY88074 is a raloxifene analog in which the basic side chain has been removed. LY88074 is an agonist of ERβ (EC50 = 232 nM).This compound stimulates uterine cell proliferation.

Cancer-Targeting Compound 1 can be used in the study of hormone-related cancers, including the treatment or prevention of fibroids, uterine leiomyomas, polycystic ovarian syndrome, or hormone-dependent Cancer, among others.

SSR126768A is a novel and selective, orally active and potent oxytocin (OT) receptor antagonist with inhibitory effects on uterine contractions for the prevention of preterm labor.

Vilaprisan (BAY 1002670) is a novel orally available and selective progesterone receptor modulator (SPRM) with antiproliferative activity against uterine fibroids (UF) and can be used for the study of uterine fibroids.

Estrogen receptor antagonist 8 acts as an estrogen receptor (ER) antagonist with anti-uterine activity and potential anti-tumorigenic activity and can be used to study ovarian dysfunction.

BLU-222 is an orally available but selective cell cycle protein-dependent kinase (CDK2) inhibitor with antitumor activity for the study of ovarian and uterine cancer.

Isoxsuprine hydrochloride (Isolait) is a beta-adrenergic agonist that causes direct relaxation of uterine and vascular smooth muscle.

Mifepristone (C-1073) is a progesterone-receptor (IC50=0.2 nM) and glucocorticoid-receptor antagonist (IC50=2.6 nM). Mifepristone is used to terminate pregnancy, treat uterine fibroids, and treat endometriosis.

Ritodrine hydrochloride (NSC 291565) binds to and activates beta-2 adrenergic receptors of myometrial cells in the uterus, which decreases the intensity and frequency of uterine contractions. Ritodrine hydrochloride (NSC 291565) is a phenethylamine derivative with tocolytic activity. Specifically, Ritodrine hydrochloride (NSC 291565) probably activates adenyl cyclase, thereby increasing production of cyclic adenosine monophosphate (cAMP), which in turn enhances the efflux of calcium from vascular smooth muscle cells. A lack of intracellular calcium prevents uterine myometrial contractions. In addition, this agent may directly inactivate myosin light chain kinase, a critical enzyme necessary for the initiation of muscle contractions.

Norethindrone (Norethisterone) is a synthetic progestational hormone with actions similar to those of PROGESTERONE but functioning as a more potent inhibitor of ovulation. It has weak estrogenic and androgenic properties. The hormone has been used in treating amenorrhea, functional uterine bleeding, endometriosis, and for contraception.

Raloxifene hydrochloride (LY156758 hydrochloride) is a second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.

Oxytocin (Syntocinon) is a mammalian neuropituitary hormone, a pleiotropic hypothalamic peptide and ligand for the oxytocin receptor, which contributes to labor, lactation, and pro-social behavior. Oxytocin has the ability to stimulate mammary secretion of breast milk, promote contraction of uterine smooth muscle during labor, and facilitate mothering.

Opigolix, a Gonadotropin-releasing hormone receptor antagonist, treats hormone-dependent conditions by inhibiting the actions of gonadotropin-releasing hormone (GnRH).