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.
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- No. CAS: 532435-68-0
- Fòrmula: C20H25NO5
- Peso molecular:359.42
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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.
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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No. CAS 532435-68-0
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Peso molecular 359.42
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CP8754 Related Classifications
HY-119080 Related Classifications
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