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Cat. No.: HY-119080

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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

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

CP8754 Chemical Structure

CAS No.: 532435-68-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

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.

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.

Chemical Information

CAS No. 532435-68-0
Molecular Weight 359.42
Formula C₂₀H₂₅NO₅
SMILES

C[C@@]12C(C=C3C(C1)=C(C)C(=O)O3)=C[C@@H](OC)[C@H](OC(NC4CC4)=O)[C@@H]2C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Tabata Y, et al. In vitro and in vivo characterization of novel nonsteroidal progesterone receptor antagonists derived from the fungal metabolite PF1092C. J Steroid Biochem Mol Biol. 2002;82(2-3):217-223. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

100 mg

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