Size | Price | Stock | Qty |
---|---|---|---|
500mg |
|
||
1g |
|
||
2g |
|
||
5g |
|
||
10g |
|
||
Other Sizes |
|
Purity: ≥98%
Estradiol cypionate (Depoestradiol; β-Estradiol 17-cypionate) is the 17 β-cyclopentylpropinate ester of estradiol used in hormone therapy for menopausal symptoms and low estrogen levels in women. It acts by inhibiting ET-1 synthesis via estrogen receptor. Estradiol cypionate is a synthetic ester of the natural estrogen, estradiol. Compared to other commonly used estradiol esters, via the intramuscular route, estradiol cypionate is found to have the longest duration of action with a duration of ~11 days, while estradiol benzoate and estradiol valerate are found to last for 4-5 days and 7-8 days, respectively.
ln Vitro |
Gastric cancer cells (MGC803, SGC7901, and BGC823) are not able to proliferate when exposed to estradiol cypionate (0-30 μM) for a period of 72 hours [4]. In the G1/S phase of gastric cancer cells (MGC803, SGC7901, and BGC823 cells), estradiol cypionate (10–25 μM) can cause cell cycle arrest and trigger apoptosis via the PI3K/Akt/mTOR pathway [4].
|
---|---|
ln Vivo |
In adolescent ovariectomized (OVX) rabbits, cortical bone density is increased by weekly intramuscular injections of estradiol cypionate (70 μg/kg) [2]. In dairy cows, the intramuscular injection of 1 mg of estradiol cypionate increases the incidence of estrus and pregnancy [3]. Estradiol cypionate (50-100mg/kg, intraperitoneal injection, every other day) inhibits tumor growth in MGC803 nude mice [4].
|
Cell Assay |
Western Blot Analysis[4]
Cell Types: MGC803, SGC7901, and BGC823 cells Tested Concentrations: 10-25 μM Incubation Duration: 48 h Experimental Results: Increased protein level of cleaved caspase-3 and PARP. diminished protein levels of AKT, p-AKT, p-mTOR, p-S6K, and p-4E-BP1. |
Animal Protocol |
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 . |
References |
[1]. Feng X, et al. NMI inhibits cancer stem cell traits by downregulating hTERT in breast cancer. Cell Death Dis. 2017 May 11;8(5):e2783.
[2]. Karimian E, et al. Resveratrol treatment delays growth plate fusion and improves bone growth in female rabbits. PLoS One. 2013 Jun 28;8(6):e67859. [3]. Sá Filho MF, et al. Impact of hormonal modulation at proestrus on ovarian responses and uterine gene expression of suckled anestrous beef cows. J Anim Sci Biotechnol. 2017 Nov 1;8:79. [4]. Qiu X, et al. Estradiol cypionate inhibits proliferation and promotes apoptosis of gastric cancer by regulating AKT ubiquitination. Biomed Pharmacother. 2023 Sep;165:115073. |
Molecular Formula |
C26H36O3
|
|
---|---|---|
Molecular Weight |
396.56
|
|
CAS # |
313-06-4
|
|
Related CAS # |
Estradiol;50-28-2;Estradiol benzoate;50-50-0;Estradiol enanthate;4956-37-0
|
|
SMILES |
C[C@@]12[C@@H](OC(CCC3CCCC3)=O)CC[C@@]1([H])[C@]4([H])CCC5=C(C=CC(O)=C5)[C@@]4([H])CC2
|
|
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
|
|
Chemical Name |
Cyclopentanepropionic acid, 3-hydroxyestra-1,3,5(10)-trien-17beta-yl ester
|
|
Synonyms |
|
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1) .This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
|
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
|
|||
---|---|---|---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.67 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 26.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.67 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 26.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.