CP8754
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.
For research use only. We do not sell to patients.
- CAS No.: 532435-68-0
- Formula: C20H25NO5
- Molecular Weight:359.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
CP8754 (10-11-10-6 M; 16-20 h) exhibits pure progesterone receptor antagonist activity in T47D-pMAMneo-LUC cells (inhibiting luciferase expression) and T47D cells (inhibiting alkaline phosphatase expression), with an IC50 of 109 nM for inhibiting alkaline phosphatase expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
CP8754 (10-60 mg/kg/day; oral administration; once daily; 5 days), when combined with progesterone, shows dose-dependent anti-progestogenic activity in an endometrial transformation model using estrogen-pretreated immature female rabbits, with lower efficacy than that of subcutaneous injection[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Immature female rabbits (800–1100 g; estrogen-primed, challenged with progesterone)[1]
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Dosage:2.5, 5, 10 mg/kg (with progesterone); 10 mg/kg (without progesterone)
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Administration:s.c.; daily; 5 days
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Result:Inhibited progesterone-induced endometrial transformation in a dose-dependent manner, showed no progestational activity when administered without progesterone.
Chemical Information
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CAS No. 532435-68-0
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Molecular Weight 359.42
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Formula C20H25NO5
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SMILES
C[C@@]12C(C=C3C(C1)=C(C)C(=O)O3)=C[C@@H](OC)[C@H](OC(NC4CC4)=O)[C@@H]2C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)