product name Estradiol valerate
Description: Estradiol valerate is a synthetic, steroidal estrogen and an estrogen ester – specifically, the 17β-valerate ester of estradiol. It acts as a prodrug of estradiol, and hence, is considered to be a natural, bioidentical form of estrogen. Along with estradiol cypionate, estradiol valerate is one of the most widely used esters of estradiol. Estradiol, or more precisely, the 17-beta-isomer of estradiol, is a human sex hormone and steroid, and the primary female sex hormone.
References: J Neurosci. 1997 Mar 1;17(5):1848-59; J Neurosci. 1992 Jul;12(7):2549-54.
356.5
Formula
C23H32O3
CAS No.
979-32-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 71 mg/mL (199.1 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19418728
| In Vitro |
In vitro activity: Estradiol (10 nM) rapidly activates sphingosine kinase isoenzyme SphK1 as determined by enhanced phosphorylation on Ser225 in MCF-7 cells. Estradiol (20 nM) stimulates rapid release of sphingosine 1-phosphate (S1P) and dihydro-S1P from MCF-7 cells. SphK1 and estrogen receptor α are mainly responsible for formation of S1P and dihydro-S1P. Down-regulation of ABCC1 or ABCG2 with siRNAs or pharmacological inhibitors decreases Estradiol (10 nM)-mediated release of S1P or dihydro-S1P from MCF-7 cells. Estradiol (10 nM) inhibits miR-21 expression in MCF-7 human breast cancer cells mediated by estrogen receptor α. Estradiol (10 nM) activates several miR-21 target gene reporters activity in MCF-7 cells through inhibiting miR-21 expression. Estradiol (10 nM) increases endogenous miR-21 target genes expression in protein but not RNA levels in MCF-7 cells. Kinase Assay: Cell Assay: |
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| In Vivo | Estradiol (80 μg/kg/day, s.c.) significantly decreases the absolute numbers of total peritoneal cell and macrophages, characterized by a double F4/80- and CD11b-positive staining, in ovariectomized C57BL/6J mice. Estradiol (80 μg/kg/day, s.c.) enhances the LPS-induced expression of proinflammatory cytokines by TGC-elicited macrophages through inhibition of PI3K activity in ovariectomized C57BL/6J mice. Proinflammatory effect of Estradiol is abolished by downregulate estrogen receptor α activity in thioglycolate-elicited macrophages. |
| Animal model | |
| Formulation & Dosage | |
| References | J Biol Chem. 2010 Apr 2;285(14):10477-86; Nucleic Acids Res. 2009 May;37(8):2584-95; J Immunol. 2010 Jul 15;185(2):1169-76. |
