MPP hydrochloride 是一种强效的选择性 ER (雌激素受体)调节剂。MPP hydrochloride 可诱导子宫内膜癌和 oLE 细胞凋亡。MPP hydrochloride 可逆转 β – 雌激素的积极作用。在体内，MPP hydrochloride 对小鼠子宫 ERalpha 具有激动剂和拮抗剂的混合作用。
MPP hydrochloride Chemical Structure
规格
价格
是否有货
数量
5 mg
￥4200
In-stock
10 mg
￥6700
In-stock
25 mg
￥13500
In-stock
50 mg
询价
100 mg
询价
* Please select Quantity before adding items.
生物活性
MPP hydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP hydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP hydrochloride reverses the positive effects of beta-estradiol. MPP hydrochloride has mixed agonist/antagonist action on murine uterine ERalphain vivo[1].
IC50 & Target
ERα
ERβ
分子量
506.04
Formula
C29H32ClN3O3
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.
溶解性数据
In Vitro:
DMSO : 250 mg/mL (494.03 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
1.9761 mL
9.8806 mL
19.7613 mL
5 mM
0.3952 mL
1.9761 mL
3.9523 mL
10 mM
0.1976 mL
0.9881 mL
1.9761 mL
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
[1]. Davis AM, et al. The effects of the selective estrogen receptor modulators, methyl-piperidino-pyrazole (MPP), and raloxifene in normal and cancerous endometrial cell lines and in the murine uterus. Mol Reprod Dev. 2006 Aug;73(8):1034-44.
MPP dihydrochloride is a highly selective estrogen receptor alpha (ERα) antagonist. MPP dihydrochloride reduces the ratio of p-ERα/ERα[1].
体外研究 (In Vitro)
MPP (1, 5, 10, 25, 50 and 100 µM; 24 h) decreases cell viability with an IC50 value of 20.01 µM in RL95-2 cells[1]. MPP dihydrochloride shows antiproliferative activity at a concentration of 10 μM in RL95-2 cells[1]. MPP dihydrochloride (20 µM; 24 h) reduces the phosphorylation of ERα, while it does not alter the phosphorylation of Akt. MPP dihydrochloride reduces the ratio of p-ERα/ERα[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
Cell Line:
RL95-2 endometrium cancer cells
Concentration:
1, 5, 10, 25, 50 and 100 µM
Incubation Time:
24 hours
Result:
The treatment with 25 µM, 50 µM and 100 µM for 24 h decreased cell viability significantly. However, cell viability was not significantly changed by MPP dihydrochloride at concentration below 25 µM.
Cell Proliferation Assay[1]
Cell Line:
RL95-2 cell
Concentration:
10, 15, 20 and 25 µM
Incubation Time:
72 hours
Result:
Showed antiproliferative activity at a concentration of 10 μM.
Western Blot Analysis[1]
Cell Line:
RL95-2 cell line
Concentration:
20 µM
Incubation Time:
24 hours
Result:
Reduced the phosphorylation of ERα, while it did not alter the phosphorylation of Akt. Reduced the ratio of p-ERα/ERα compared to the control group.
体内研究 (In Vivo)
MPP (Low dose 20 μg/kg body weight or high dose 200 μg/kg body weight) leads to a dose-dependent attenuation of percent prepulse inhibition (PPI)[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male C57BL/6N mice at the age of 9-10 weeks[2]
Dosage:
Low dose (20 μg/kg body weight) or high dose (200 μg/kg body weight)
Administration:
Administered subcutaneously (s.c.) injected; injection volume of 5 mL/kg; 60 min before PPI testing
Result:
Led to a dose-dependent attenuation of percent PPI. Pretreatment with 200 μg/kg reduced the mean percent PPI scores by ~30%.
分子量
542.50
Formula
C29H33Cl2N3O3
CAS 号
911295-24-4
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Karaboğa Arslan AK, et al. α-Chaconine and α-Solanine Inhibit RL95-2 Endometrium Cancer Cell Proliferation by Reducing Expression of Akt (Ser473) and ERα (Ser167). Nutrients. 2018 May 25;10(6). pii: E672.
[2]. Labouesse MA, et al. Effects of selective estrogen receptor alpha and beta modulators on prepulse inhibition in male mice. Psychopharmacology (Berl). 2015 Aug;232(16):2981-94.
