ER/Estrogen receptor. Estradiol enanthate is a long-acting estrogen ester used in combination with dihydroxyprogesterone acetophenide (DHPA) as a once-monthly injectable contraceptive. No specific binding affinity or potency data (e.g., IC₅₀, EC₅₀) were reported in this study. [1]

避孕效果：在一项纳入365名青少年（14-19岁）的前瞻性、开放性、随机研究中，使用含戊酸雌二醇 10 mg和双羟孕酮醋酸酯150 mg的每月一次注射用避孕药，在12个使用周期内共发生5例妊娠：第1组（每30±3天注射一次）2例，第2组（于月经周期第7-10天注射）3例，差异无统计学意义(p = 0.48)。生命表分析显示，第1组和第2组的累积妊娠率分别为1.4%和1.7%。[1]
出血模式：第1组平均出血天数为5.8 ± 1.7天，第2组为5.5 ± 1.2天(p = 0.187)。平均周期长度为第1组28.7 ± 4.1天，第2组26.6 ± 3.8天(p < 0.001)。在90天分段分析中，第1组点滴出血天数为2.0 ± 1.0至3.5 ± 6.0天，第2组为2.3 ± 1.2至3.6 ± 2.3天，组间差异无统计学意义。[1]
治疗完成率：365名入组受试者中，266名（73%）完成了12个月治疗：第1组130/186（70%），第2组136/179（76%）（p = 0.21）。第1组平均研究时长为7.64 ± 0.5个月，第2组为7.55 ± 0.4个月。[1]
引言：本研究比较了两种每月注射一次的避孕药方案，其中含有150mgdihydroxyprogesterone acetophenide和10mgestradiol enanthate（Perlutan），使用周期为12个周期。 方法：将365名青少年随机分为两组。第1组的患者在月经周期的第1-5天首次注射Perlutan，随后每30+/-3天注射一次，而第2组的患者则遵循传统的给药时间表，即第一次注射在月经周期第7天至第10天之间，随后在停药出血第1天后7-10天注射。此时间表可能会导致注射时间不规则。 结果：两组在耐受性或妊娠方面没有显著差异（第1组2例，第2组3例）。 结论：每月给药将年度注射次数限制在最多12次，从而经常减少年度总剂量，同时保持与传统方案相似的疗效和耐受性。

Study Design: This was a prospective, open, randomized clinical study conducted at six research centers in Brazil. A total of 365 female adolescents aged 14–19 years were enrolled and randomized into two groups. [1]

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Dosing Regimen: Estradiol enanthate (10 mg) was administered intramuscularly as part of a combination injectable contraceptive (Perlutan®) containing dihydroxyprogesterone acetophenide 150 mg. Group 1 received the first injection between days 1–5 of the menstrual cycle, with subsequent injections every 30 ± 3 days. Group 2 received the first injection between days 7–10 of the menstrual cycle, with subsequent injections scheduled 7–10 days after the first day of withdrawal bleeding. All injections were given deeply intramuscularly. [1]
Duration: The study duration was 12 cycles (approximately 12 months) of contraceptive use. [1]
Exclusion Criteria: Patients were excluded if they had used any hormonal contraception in the preceding 3–8 months, had known neoplastic disease, serious hepatopathy, kidney insufficiency, hypersensitivity to any component, were pregnant or lactating, amenorrheic, or had contraindications to hormonal contraception. [1]
Monthly injectable steroid contraceptives which contained the long-acting progestogen dihydroxyprogesterone acetofenide plus a shorter-acting estrogen (usually estradiol enanthate) were used by women in two of the countries (Chile and Mexico) from which data were collected. In preliminary analyses of data from Chile (1979-1983), a strong association was observed between use of these products and invasive cervical cancer. Therefore, three additional data sets from these two countries were analyzed in further detail for this report. Analyses of additional data from Chile on invasive cervical cancer (1983-1985) and cervical carcinoma in situ (1979-1986) and of data on invasive cervical cancer from Mexico (1979-1986) failed to confirm the initially observed association. The original finding was probably due to chance, but a causal interpretation cannot be confidently ruled out, and additional studies are warranted.[2]

Adverse Events: The incidence of nonserious adverse events possibly related to the study drug was 26.9% in Group 1 and 20.7% in Group 2 (p = 0.22). Four serious adverse events were reported (influenza-like symptoms, pneumonia, cholecystectomy, and acute diarrhea), but none were considered by investigators to be related to the study medication. [1]
Weight Change: Mean body weight increased by 1.1 kg in Group 1 and 0.9 kg in Group 2 over the study duration (p = 0.931). The weight change was not significantly different between groups. [1]
Blood Pressure and Pulse Rate: No statistically significant changes in systolic blood pressure, diastolic blood pressure, or pulse rate were observed in either group during the study. [1]
Dysmenorrhea: There was no difference between the two groups regarding the occurrence of moderate to severe dysmenorrhea, reported by 24/175 patients in Group 1 and 23/175 in Group 2. [1]
Discontinuation Reasons: Discontinuation due to bleeding problems occurred in 0.7% of Group 1 and 2.0% of Group 2 (p not significant). Discontinuation due to personal reasons was 7.1% in Group 1 and 1.3% in Group 2 (p < 0.05). [1]

[1]. Comparison of two regimens of a monthly injectable contraceptive containing dihydroxyprogesterone acetophenide and estradiol enanthate. Contraception. 2006;73(3):249-252.

[2]. Monthly injectable steroid contraceptives and cervical carcinoma. Am J Epidemiol. 1989;130(2):237-247.

Background and Composition: Estradiol enanthate is a long-acting estrogen ester that, in combination with dihydroxyprogesterone acetophenide (150 mg), forms a once-monthly injectable contraceptive marketed as Perlutan®. The combination is widely used in Latin America, with over 6 million units administered annually in Brazil alone. [1]
Mechanism of Action: The combination of estradiol enanthate and dihydroxyprogesterone acetophenide inhibits ovulation by suppressing gonadotropin secretion. Monthly withdrawal bleeding occurs approximately 3 weeks after injection, providing users with reassurance of contraceptive efficacy and mimicking natural menstruation. [1]
Dose Alternatives: A lower-dose formulation containing estradiol enanthate 6 mg and dihydroxyprogesterone acetophenide 90 mg has been proposed for women with low body weight (53 kg or less), demonstrating comparable efficacy to the higher-dose formulation. [1]
Clinical Application: The study demonstrates that the monthly administration schedule (injection every 30 ± 3 days) is as effective and acceptable as the traditional schedule based on withdrawal bleeding timing. Monthly administration limits annual injections to a maximum of 12, potentially reducing the total annual dose while maintaining efficacy. [1]
Estradiol enanthate is a steroid ester.

C25H36O3

384.55

384.266

4956-37-0

Estradiol;50-28-2;Estradiol (cypionate);313-06-4;Estradiol benzoate;50-50-0

21070

White to off-white solid powder

1.1±0.1 g/cm3

509.5±50.0 °C at 760 mmHg

94-96ºC

197.1±22.9 °C

0.0±1.4 mmHg at 25°C

1.560

7.68

46.53

1

3

7

28

546

5

CCCCCCC(=O)O[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CCC4=C3C=CC(=C4)O)C

RFWTZQAOOLFXAY-BZDYCCQFSA-N

InChI=1S/C25H36O3/c1-3-4-5-6-7-24(27)28-23-13-12-22-21-10-8-17-16-18(26)9-11-19(17)20(21)14-15-25(22,23)2/h9,11,16,20-23,26H,3-8,10,12-15H2,1-2H3/t20-,21-,22+,23+,25+/m1/s1

[(8R,9S,13S,14S,17S)-3-hydroxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl] heptanoate

ESTRADIOL ENANTHATE; 4956-37-0; Oestradiol 17-heptanoate; Estradiol Enantate; Estradiol 17-heptanoate; Estradiol enanthate [USAN]; SQ 16,150; PAP315WZIA;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中（例如氮气保护），避免吸湿/受潮和光照。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO: 125 mg/mL (325.06 mM)

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。