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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
80 Results for "
human estrogen receptors
" in MedChemExpress (MCE) Product Catalog:
Products (80)
80 Results for "human estrogen receptors" in MCE Product Catalog:
6
6 Publications Verification
Synonyms: GDC-9545; RG6171
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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 .
6
6 Publications Verification
Synonyms: 17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate
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Hydroxyprogesterone caproate (17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate) is a progesterone receptor (progesterone receptor) ligand and steroid hormone transcription inhibitor. Hydroxyprogesterone caproate downregulates estrogen receptors in target tissues and activates their metabolic pathways, and exhibits equivalent affinity for progesterone receptor A and progesterone receptor B. Hydroxyprogesterone caproate shows no consistent teratogenicity or developmental toxicity in rat, mouse and monkey models, but induces resorption or abortion in rhesus monkeys at human-equivalent doses. Hydroxyprogesterone caproate promotes the production of TNF-α in lipopolysaccharide-stimulated whole blood from non-pregnant women. Hydroxyprogesterone caproate can be used in scientific research related to preterm birth .
5
5 Cited Publications
Synonyms: Clomifene; (Z/E)-Enclomiphene; (Z/E)-Enclomifene
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Clomiphene (Clomifene; (Z/E)-Enclomiphene; (Z/E)-Enclomifene) is an orally active ovulation-inducing agent. Clomiphene binds to hypothalamic estrogen receptors to elevate FSH levels, and exhibits antiestrogenic or estrogenic properties. Clomiphene can induce erturbations during meiotic maturation and cytogenetic abnormalities in mouse oocytes. Clomiphene ameliorates memory impairment in PCOS models. Clomiphene mobilizes cytosolic calcium and reduces viability in prostate cancer cells. Clomiphene can be used for the research of polycystic ovary syndrome (PCOS) and prostate cancer .
4
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Prinaberel (ERB-041) is a potent and selective estrogen receptor (ER) β agonist with IC50s of 5.4, 3.1 and 3.7 nM for human, rat and mouse ERβ, respectively. Prinaberel displays >200-fold selectivity for ERβ over ERα. Prinaberel is a potent skin cancer chemopreventive agent that acts by dampening the WNT/β-catenin signaling pathway. Prinaberel induces ovarian cancer apoptosis .
3
3 Cited Publications
Cat. No.: HY-18719
CAS No.: 112093-28-4
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Endoxifen Z-isomer is an orally active selective PKCβ1 inhibitor with an IC50 of 360 nM against human PKCβ1. Endoxifen Z-isomer also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. Endoxifen Z-isomer can be used in research related to ER + breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors .
3
3 Cited Publications
Cat. No.: HY-18719A
CAS No.: 1032008-74-4
Endoxifen Z-isomer hydrochloride is an orally active selective PKCβ1 inhibitor with an IC50 of 360 nM against human PKCβ1. It also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer hydrochloride binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer hydrochloride inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. It can be used in research related to ER + breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors .
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1
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Diisopropyl phthalate (DiPP) is a phthalate diester, which is widely used as an additive in plastics and consumer products. Diisopropyl phthalate has a weak binding ability to the recombinant human estrogen receptor, with an IC50 of 41000 μM .
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Perfluorobutanesulfonic acid (PFBS) is a short-chain perfluoroalkyl substance and the main replacement for perfluorooctanesulfonic acid. Perfluorobutanesulfonic acid induces fat accumulation in human HepG2 hepatoma cells. Perfluorobutanesulfonic acid promotes lipid accumulation by activating PPARγ pathway and triggering oxidative stress, endoplasmic reticulum stress and calcium dyshomeostasis. Perfluorobutanesulfonic acid impairs reproduction and causes developmental disorders in offspring of Caenorhabditis elegans. Perfluorobutanesulfonic acid disrupts pancreatic organogenesis and lipid homeostasis in zebrafish embryos. Perfluorobutanesulfonic acid can be used in environmental toxicology, lipid metabolism and developmental toxicity studies .
Category:
Flavonols other families Flavonoids Metabolic Disease Phenols Polyphenols Plants Disease Research Fields
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Cat. No.: HY-153468
CAS No.: 3035547-78-2
Synonyms: TEQ103; Sera2
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ErSO-TFPy (TEQ103) is an ERα+ tumor cell inhibitor with low nanomolar cytotoxic activity against ERα+ breast cancer cells. ErSO-TFPy activates the sodium channel TRPM4, causes an imbalance of intracellular calcium and sodium ions. ErSO-TFPy dysregulates calcium homeostasis in ERα+ tumor cells, triggers the anticipatory unfolded protein response, and induces rapid immune cell-independent necrotic cell death. ErSO-TFPy can be used for the research of estrogen receptor alpha positive breast cancer .
Cat. No.: HY-164159
CAS No.: 130603-71-3
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α-Glucosylrutin, a flavonoid, is a potent antioxidant with free radical scavenging activity. α-Glucosylrutin reduces MMP-1 gene expression, protein expression, and enzyme activity, and reduces MMP-2 protein expression and enzyme activity in UVA-irradiated human dermal fibroblasts. α-Glucosylrutin prevents oxidative stress-induced intracellular tyrosine residue phosphorylation and counteracts intracellular thiol level depletion in human skin cells. α-Glucosylrutin is effective in the prevention of dermatologic diseases in which oxidative stress is of pathogenetic relevance, e.g. in polymorphous light eruption (PLE). α-Glucosylrutin can be used for the research of UV-induced skin photodamage/photoaging .
Cat. No.: HY-B0652
CAS No.: 54048-10-1
Synonyms: 3-Oxodesogestrel; 3-keto-Desogestrel
Cat. No.: HY-N4119
CAS No.: 13241-32-2
Category:
other families Flavonoids Flavonones Phenols Polyphenols Plants
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Paroxypropione (4'-Hydroxypropiophenone) is a manufactured, nonsteroidal estrogen and can be used for endocrine research .
Cat. No.: HY-B0110
CAS No.: 60282-87-3
Synonyms: SHB 331; WL 70
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Progesterone Receptor ERK Cytochrome P450 Protease Activated Receptor (PAR) 5 alpha Reductase MMP Drug Intermediate
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Gestodene (SHB 331; WL 70) is an orally active synthetic progestogen compound of the 19-nortestosterone class. Gestodene binds with high affinity to the progesterone receptor, inhibits 5α-reductase, binds to androgen and aldosterone receptors, and inactivates CYP3A. Gestodene acts as a positive allosteric modulator of PAR1, enhances PAR1-mediated signaling pathways, and is capable of increasing the activation potency of PAR1-AP toward PAR1, thereby promoting ERK1/2 phosphorylation, receptor internalization, cell morphological changes, and human platelet aggregation. Gestodene and its A-ring reduced metabolites promote the proliferation, differentiation, and mineralization of neonatal rat osteoblasts. Gestodene itself has no binding capacity for estrogen receptors, and this osteogenic activity depends on intracellular metabolism to generate A-ring reduced products with estrogen-like agonistic activity. Gestodene is useful for research on diseases related to progesterone secretion and diseases related to thrombosis .
Synonyms: Piperazine estrone sulfate; Estrone sulfate piperazine salt
Cat. No.: HY-W013807
CAS No.: 109-43-3
Synonyms: Dibutyl decanedioate
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Dibutyl sebacate (Dibutyl decanedioate) is a PVC eco-friendly plasticizer. Dibutyl sebacate plasticizes Eudragit RS 30D, reducing the glass transition temperature and minimum film-forming temperature for sustained-release coatings, with no aging effect .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
