2. Vitamin D Related/Nuclear Receptor
  3. Progesterone Receptor
  4. CP8754

CP8754 是一种口服有效、选择性人类孕酮受体（hPR）拮抗剂，可阻断孕酮介导的信号通路。CP8754 竞争性抑制 [3H]-孕酮与 hPR 的结合，体外可抑制孕酮依赖的外源性荧光素酶和内源性碱性磷酸酶表达，体内可抑制兔子宫内膜转化。CP8754 不与人类糖皮质激素受体（hGR）、雌激素受体（hER）及大鼠雄激素受体（rAR）显著结合。CP8754 可用于乳腺癌、子宫内膜异位症、子宫肌瘤、脑膜瘤等孕激素相关疾病，以及激素依赖性肿瘤的研究 。

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CP8754

CP8754 Chemical Structure

CAS No. : 532435-68-0

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CP8754 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

CP8754 (10-11-10-6 M；16-20 h) 在 T47D-pMAMneo-LUC 细胞 (抑制荧光素酶表达) 和 T47D 细胞 (抑制碱性磷酸酶表达) 中表现出纯孕酮受体拮抗活性，抑制碱性磷酸酶表达的 IC50 为 109 nM[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CP8754 相关抗体:
体内研究
(In Vivo)

CP8754 (2.5-10 mg/kg；皮下注射；每日一次；连续 5 天) 在雌激素预处理并经孕酮激发的未成熟雌性家兔中表现出剂量依赖性抗孕激素活性[1]。
CP8754 (10-60 mg/kg/ 天；口服；每日一次；5 天) 在雌激素预处理的未成年雌性兔子宫内膜转化模型中，与孕酮联合使用时，呈剂量依赖性抗孕激素活性，但其效力低于皮下注射[1]。

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.
分子量

359.42

Formula

C20H25NO5
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CP8754 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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目录号：
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