2. Vitamin D Related/Nuclear Receptor
  3. Progesterone Receptor
  4. 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.

CP8754

CP8754 Chemical Structure

CAS No. : 532435-68-0

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CP8754 Related Antibodies

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Description

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[1].

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.

CP8754 Related Antibodies
In Vivo

CP8754 (2.5-10 mg/kg; subcutaneous injection; once daily; for 5 consecutive days) shows dose-dependent anti-progestogenic activity in immature female rabbits pretreated with estrogen and challenged with progesterone[1].
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.

Animal Model: Immature female rabbits (800–1100 g; estrogen-primed, challenged with progesterone)[1]
Dosage: 2.5, 5, 10 mg/kg (with progesterone); 10 mg/kg (without progesterone)
Administration: s.c.; daily; 5 days
Result: Inhibited progesterone-induced endometrial transformation in a dose-dependent manner, showed no progestational activity when administered without progesterone.
Molecular Weight

359.42

Formula

C20H25NO5
CAS No.
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CP8754 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CP8754532435-68-0CP 8754CP-8754Progesterone ReceptorNR3C3immature female rabbitshuman progesterone receptorhuman estrogen receptorshuman glucocorticoid receptorshGRrat androgen receptorsT47D-pMAMneo-LUC cellsrARhPRhERT47D cellshuman mammary carcinoma cellsInhibitorinhibitorinhibit

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