| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| 5g |
|
||
| 10g |
|
||
| Other Sizes |
|
| 靶点 |
ER
|
|---|---|
| 体外研究 (In Vitro) |
当暴露于环丙酸雌二醇 (0-30 μM) 72 小时时，胃癌细胞（MGC803、SGC7901 和 BGC823）无法增殖 [4]。在胃癌细胞（MGC803、SGC7901 和 BGC823 细胞）的 G1/S 期，环戊丙酸雌二醇 (10–25 μM) 可通过 PI3K/Akt/mTOR 途径引起细胞周期停滞并引发细胞凋亡 [4]。
|
| 体内研究 (In Vivo) |
在青春期卵巢切除 (OVX) 兔子中，每周肌内注射环戊丙酸雌二醇 (70 μg/kg) 可增加皮质骨密度 [2]。在奶牛中，肌肉注射1mg环戊丙酸雌二醇会增加发情和妊娠的发生率[3]。环丙酸雌二醇（50-100mg/kg，腹腔注射，每隔一天）抑制MGC803裸鼠肿瘤生长[4]。
|
| 酶活实验 |
环戊丙酸雌二醇（Depoestradiol；Estradiol cypionate; β-雌二醇 17-环戊丙酸酯）通过调节AKT泛素化抑制癌症增殖和促进细胞凋亡：癌症是世界范围内常见的胃肠道恶性肿瘤，死亡率高，预后差。多药耐药性仍然是患者成功治疗的主要障碍。因此，开发新的疗法来增强抗肿瘤作用具有重要意义。在本研究中，我们在体外和体内研究了Estradiol cypionate（ECP）对癌症的影响。我们的数据表明，ECP抑制癌症细胞的增殖，促进细胞凋亡，并导致G1/S期阻滞。ECP促进癌症细胞凋亡的机制与AKT泛素化修饰水平升高引起的AKT蛋白表达下调有关，最终抑制PI3K-AKT-mTOR信号通路的过度激活。体内肿瘤发生实验表明，ECP能显著抑制癌症细胞的生长，具有临床应用前景。上述结果表明，ECP通过PI3K/Akt/mTOR途径抑制癌症的生长并诱导细胞凋亡。总之，我们数据中显示的疗效表明，ECP是一种治疗癌症的有前途的抗肿瘤化合物[4]。
|
| 细胞实验 |
蛋白质印迹分析[4]
细胞类型： MGC803、SGC7901 和 BGC823 细胞 测试浓度： 10-25 μM 孵育持续时间： 48 小时 实验结果： 裂解 caspase-3 和 PARP 的蛋白质水平增加。 AKT、p-AKT、p-mTOR、p-S6K 和 p-4E-BP1 的蛋白质水平降低。 |
| 动物实验 |
Animal/Disease Models: MGC803 nude mice tumor model[4].
Doses: 50-100 mg/kg Route of Administration: ip, every other day Experimental Results: Inhibited tumor growth. Increased Cleaved caspase-3 expression, diminished Ki67, AKT and p-AKT in tumors . |
| 药代性质 (ADME/PK) |
Absorption, Distribution and Excretion
When conjugated with aryl and alkyl groups for parenteral administration, the rate of absorption of oily preparations is slowed with a prolonged duration of action, such that a single intramuscular injection of estradiol valerate or estradiol cypionate is absorbed over several weeks. Estradiol, estrone and estriol are excreted in the urine along with glucuronide and sulfate conjugates. The distribution of exogenous estrogens is similar to that of endogenous estrogens. Estrogens are widely distributed in the body and are generally found in higher concentrations in the sex hormone target organs. Metabolism / Metabolites Exogenous estrogens are metabolized in the same manner as endogenous estrogens. Circulating estrogens exist in a dynamic equilibrium of metabolic interconversions. These transformations take place mainly in the liver. Estradiol is converted reversibly to estrone, and both can be converted to estriol, which is the major urinary metabolite. Estrogens also undergo enterohepatic recirculation via sulfate and glucuronide conjugation in the liver, biliary secretion of conjugates into the intestine, and hydrolysis in the gut followed by reabsorption. In postmenopausal women, a significant proportion of the circulating estrogens exist as sulfate conjugates, especially estrone sulfate, which serves as a circulating reservoir for the formation of more active estrogens. |
| 毒性/毒理 (Toxicokinetics/TK) |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Estradiol cypionate has not been studied during breastfeeding. However, a similar drug, estradiol valerate, has been used to suppress lactation, usually in combination with testosterone. Generally, estradiol cypionate should be avoided in mothers wishing to breastfeed, especially if started before the milk supply is well established at about 6 weeks postpartum. The decrease in milk supply can happen over the first few days of estrogen exposure. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Another injection ester form of estradiol, estradiol valerate was previously used therapeutically to suppress lactation, usually in combination with testosterone. A retrospective cohort study compared 371 women who received high-dose estrogen (either 3 mg of diethylstilbestrol or 150 mcg of ethinyl estradiol daily) during adolescence for adult height reduction to 409 women who did not receive estrogen. No difference in breastfeeding duration was found between the two groups, indicating that high-dose estrogen during adolescence has no effect on later breastfeeding. Protein Binding Estrogens circulate in the blood largely bound to sex hormone binding globulin (SHBG) and albumin. |
| 参考文献 |
|
| 其他信息 |
Pharmacodynamics
Estrogen mediates its effects across the body through potent agonism of the Estrogen Receptor (ER), which is located in various tissues including in the breasts, uterus, ovaries, skin, prostate, bone, fat, and brain. Estradiol binds to both subtypes of the Estrogen Receptor: Estrogen Receptor Alpha (ERα) and Estrogen Receptor Beta (ERβ). Estradiol also acts as a potent agonist of G Protein-coupled Estrogen Receptor (GPER), which has recently been recognized as a major mediator of estradiol's rapid cellular effects. |
| 分子式 |
C26H36O3
|
|
|---|---|---|
| 分子量 |
396.56
|
|
| 精确质量 |
396.266
|
|
| 元素分析 |
C, 78.75; H, 9.15; O, 12.10
|
|
| CAS号 |
313-06-4
|
|
| 相关CAS号 |
Estradiol;50-28-2;Estradiol benzoate;50-50-0;Estradiol enanthate;4956-37-0; Alpha-Estradiol;57-91-0;Estradiol (Standard);50-28-2;Estradiol-d3;79037-37-9;Estradiol-d4;66789-03-5;Estradiol-d5;221093-45-4;Estradiol-13C2;82938-05-4;Estradiol (cypionate);313-06-4;Estradiol benzoate;50-50-0;Estradiol enanthate;4956-37-0;Estradiol hemihydrate;35380-71-3;Estradiol-d2;53866-33-4;Estradiol-13C6;Estradiol-d2-1;3188-46-3;rel-Estradiol-13C6; 979-32-8 (valerate); 113-38-2 (dipropionate); 57-63-6 (ethinyl); 172377-52-5 (sulfamate); 3571-53-7 (undecylate)
|
|
| PubChem CID |
9403
|
|
| 外观&性状 |
White to off-white solid powder
|
|
| 密度 |
1.2±0.1 g/cm3
|
|
| 沸点 |
532.8±50.0 °C at 760 mmHg
|
|
| 熔点 |
≥300 °C(lit.)
|
|
| 闪点 |
207.7±22.9 °C
|
|
| 蒸汽压 |
0.0±1.5 mmHg at 25°C
|
|
| 折射率 |
1.579
|
|
| LogP |
7.59
|
|
| tPSA |
46.53
|
|
| 氢键供体(HBD)数目 |
1
|
|
| 氢键受体(HBA)数目 |
3
|
|
| 可旋转键数目(RBC) |
5
|
|
| 重原子数目 |
29
|
|
| 分子复杂度/Complexity |
597
|
|
| 定义原子立体中心数目 |
5
|
|
| SMILES |
C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2OC(=O)CCC4CCCC4)CCC5=C3C=CC(=C5)O
|
|
| InChi Key |
UOACKFBJUYNSLK-XRKIENNPSA-N
|
|
| InChi Code |
InChI=1S/C26H36O3/c1-26-15-14-21-20-10-8-19(27)16-18(20)7-9-22(21)23(26)11-12-24(26)29-25(28)13-6-17-4-2-3-5-17/h8,10,16-17,21-24,27H,2-7,9,11-15H2,1H3/t21-,22-,23+,24+,26+/m1/s1
|
|
| 化学名 |
Cyclopentanepropionic acid, 3-hydroxyestra-1,3,5(10)-trien-17beta-yl ester
|
|
| 别名 |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month 注意： (1). 本产品在运输和储存过程中需避光。 (2). 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。 |
|
| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| 溶解度 (体外实验) |
|
|||
|---|---|---|---|---|
| 溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 2.67 mg/mL (6.73 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 26.7 mg/mL的澄清DMSO储备液加入到400 μL PEG300中并混合均匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。 *生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。 配方 2 中的溶解度: ≥ 2.67 mg/mL (6.73 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。 例如，若需制备1 mL的工作液，可将 100 μL 26.7 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。 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。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5217 mL | 12.6084 mL | 25.2169 mL | |
| 5 mM | 0.5043 mL | 2.5217 mL | 5.0434 mL | |
| 10 mM | 0.2522 mL | 1.2608 mL | 2.5217 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
计算结果:
工作液浓度： mg/mL；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
ET receptor antagonist 1
ERα degrader 6
hFSH-β-(33-53) (TFA)
Bisphenol AF-d4 (BPAF-d4; 4,4'-(Perfluoropropane-2,2-diyl)diphenol-d4)
InvivoChem的所有产品仅用于作科学研究，不面向患者销售
Copyright 2020 InvivoChem LLC | All Rights Reserved 粤ICP备20063088号-1
COA
粤公网安备 44011102003439号