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。
| 生物活性 | MPP hydrochloride is a potent and selectiveER (estrogen receptor)modulator. MPP hydrochloride induces significantapoptosisin the endometrialcancerand oLE cell lines. MPP hydrochloride reverses the the positive effects ofbeta-estradiol. MPP hydrochloride has mixed agonist/antagonist action on murine uterineERalphain vivo[1]. |
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体外研究
(In Vitro) | MPP (1, 5, 10, 25, 50 and 100 μM; 24 h) decreases cell viability with an IC50value 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].
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 endometrium cancer cells | | 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 endometrium cancer cells | | 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. |
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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].
| 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%. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(494.03 mM;Need ultrasonic) 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 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： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.11 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (4.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.11 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.11 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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