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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 532435-68-0
分子式: C₂₀H₂₅NO₅
分子量:359.42

保管条件:

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

Data Sheet (274 KB)

CP8754 構造式

CAS 番号: 532435-68-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

生物活性

製品説明

体外実験

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.

体内実験

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.

化学情報

CAS 番号 532435-68-0
分子量 359.42
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (274 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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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