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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
26 Results for "
rat estrogen receptor
" in MedChemExpress (MCE) Product Catalog:
Products (26)
26 Results for "rat estrogen receptor" in MCE Product Catalog:
6
6 Publications Verification
Synonyms: GDC-9545; RG6171
Target:
Research Areas:
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 .
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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 .
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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 .
Cat. No.: HY-N6043
CAS No.: 69039-02-7
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AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender selective neuroprotective effects in a male rat model of Parkinson's disease .
Cat. No.: HY-B0110
CAS No.: 60282-87-3
Synonyms: SHB 331; WL 70
Target:
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 .
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 .
Synonyms: 17α-Hydroxyprogesterone hexanoate(Standard); 17α-Hydroxyprogesterone caproate (Standard)
Research Areas:
Hydroxyprogesterone caproate (Standard) is the analytical standard of Hydroxyprogesterone caproate. This product is intended for research and analytical applications. 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 .
Cat. No.: HY-W013807R
CAS No.: 109-43-3
Synonyms: Dibutyl decanedioate (Standard)
Research Areas:
Dibutyl sebacate (Standard) (Dibutyl decanedioate (Standard)) is the analytical standard of Dibutyl sebacate (HY-W013807). This product is intended for research and analytical applications. 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 .
Cat. No.: HY-123163
CAS No.: 240805-96-3
Synonyms: RWJ-66826; RTI-6617-003
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JNJ-1250132 (RWJ-66826) is an orally active and potent steroidal progesterone receptor (PR) antagonist, with an IC50 of 1.3 nM. JNJ-1250132 inhibits binding of the receptor to DNA in vitro. JNJ-1250132 is a potent competitive inhibitor of binding to the human glucocorticoid receptor (GR) (IC50=0.50 nM) and the rat androgen receptor (AR) (IC50=5.6 nM), and was a weak inhibitor of binding to human Estrogen receptor (ER) (IC50 >3000 nM) .
Cat. No.: HY-135903
CAS No.: 2407529-33-1
Synonyms: GDC-9545 tartrate; RG6171 tartrate
Target:
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 .
Cat. No.: HY-135671
CAS No.: 118174-38-2
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AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus .
Cat. No.: HY-B0110R
CAS No.: 60282-87-3
Synonyms: SHB 331 (Standard); WL 70 (Standard)
Gestodene (Standard) (SHB 331 (Standard); WL 70 (Standard)) is the analytical standard of Gestodene (HY-B0110). This product is intended for research and analytical applications. Gestodene 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 .
Cat. No.: HY-B0110S
CAS No.: 1542211-40-4
Synonyms: SHB 331-d6; WL 70-d6
Gestodene-d6 (SHB 331-d6; WL 70-d6) is the deuterated-labeled Gestodene (HY-B0110). Gestodene 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 .
Cat. No.: HY-W753897
Synonyms: SHB 331-d7; WL 70-d7
Gestodene-d7 (SHB 331-d7; WL 70-d7) is the deuterated-labeled Gestodene (HY-B0110). Gestodene 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 .
Cat. No.: HY-123664
CAS No.: 68307-81-3
Synonyms: LY133314
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Research Areas:
Trioxifene mesylate (LY133314) is an orally active and selective estrogen receptor (ER) modulator with human ERα IC50 of 203.49 nM and Ki of 20.84 nM. Trioxifene mesylate binds estradiol receptors, inhibits ERα-mediated gene expression, reduces circulating gonadotrophin levels. Trioxifene mesylate can be used for the research of advanced breast cancer and androgen-independent, metastatic prostatic adenocarcinoma .
Synonyms: ent-β-Estradiol; ent-17β-Estradiol; ent-17β-Oestradiol
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Ent-Estradiol is the enantiomer of Estradiol (HY-B0141). Ent-Estradiol is a highly selective estrogen receptor ligand, but does not possess estrogenic activity. Ent-Estradiol displays IC50 values of 24.9 nM, 9.59 nM and 8.17 nM for human, rat and mouse ERβ, and 151 nM, 246 nM and 268 nM for human, rat and mouse ERα, respectively. Ent-Estradiol can be used for the study of menopausal physiological changes .
Cat. No.: HY-119080
CAS No.: 532435-68-0
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CP8754 is an orally active, selective human progesterone receptor (hPR) antagonist that blocks progesterone-mediated signaling pathways. CP8754 competitively inhibits the binding of [ 3H]-progesterone to hPR. And in vitro, CP8754 inhibits progesterone-dependent exogenous luciferase and endogenous alkaline phosphatase expression; while in vivo, CP8754 inhibits rabbit endometrial transformation. CP8754 does not significantly bind to human glucocorticoid receptors (hGR), estrogen receptors (hER), or rat androgen receptors (rAR). CP8754 can be used in the study of progesterone-related diseases such as breast cancer, endometriosis, uterine fibroids, and meningioma, as well as hormone-dependent tumors .
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6α-Fluorotestosterone is a non-aromatizable aromatase inhibitor, with IC50 values of 115 nM and 580 nM against human and rat aromatase, respectively. 6α-Fluorotestosterone binds to the substrate site of human aromatase P450arom with a Ki of 150 nM, but is not aromatized into estrogen. In vivo, 6α-Fluorotestosterone maintains sexual behavior in castrated male rats (with an effect comparable to that of testosterone), induces defeminization of sexual development, and inhibits nuclear translocation of hypothalamic estrogen receptors; its pro-mating effect is blocked by the aromatase inhibitors ATD and Fadrozole (HY-14247A). Combined with Progesterone (HY-N0437), 6α-Fluorotestosterone induces lordosis behavior in ovariectomized female rats. 6α-Fluorotestosterone can be used in studies related to anovulatory infertility and sexual behavior regulation .
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Tamoxifen derivative-1 is a derivative of Tamoxifen (HY-13757A) with reduced affinity for estrogen receptor (ER). Tamoxifen derivative-1 blocks estrogen-induced activity, inhibits estrogen-stimulated uterine growth, and exhibits uterotrophic activity in immature rats. Tamoxifen derivative-1 can be used in research related to breast cancer .
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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
