CAS NO: | 979-32-8 |
规格: | ≥98% |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
1g | 电议 |
5g | 电议 |
10g | 电议 |
Molecular Weight (MW) | 356.5 |
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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 | |
Other info | Chemical Name: (17β)-3-hydroxyestra-1,3,5(10)-trien-17-yl valerate InChi Key: RSEPBGGWRJCQGY-RBRWEJTLSA-N InChi Code: InChI=1S/C23H32O3/c1-3-4-5-22(25)26-21-11-10-20-19-8-6-15-14-16(24)7-9-17(15)18(19)12-13-23(20,21)2/h7,9,14,18-21,24H,3-6,8,10-13H2,1-2H3/t18-,19-,20+,21+,23+/m1/s1 SMILES Code: CCCCC(O[C@H]1CC[C@@]2([H])[C@]3([H])CCC4=C(C=CC(O)=C4)[C@@]3([H])CC[C@]12C)=O |
Synonyms | Estraval; Progynova; Valergen; Altadiol; Deladiol; Delestrogen; oestradiol valerate; |
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. |
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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 | Mice |
Formulation & Dosage | 80 μg/kg/day, s.c. |
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. |