
Epiallopregnanoloneinactive as a GABAA receptor modulator and used as a control substance to examine GABA neurotransmission. |
Sample solution is provided at 25 µL, 10mM.
































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Cas No. | 567-01-1 | SDF | Download SDF |
Synonyms | 5α-Pregnan-20-one,3β,21-dihydroxy-5α-Pregnan-20-one,3β,5α-Tetrahydrodeoxycorticosterone,3β,5α-Tetrahydroprogesterone | ||
Chemical Name | 3,21-dihydroxy-, (3ß,5α)-pregnan-20-one | ||
Canonical SMILES | C[C@@]12[C@](CC[C@@H]2C(CO)=O)([H])[C@]3([H])CC[C@@]4([H])C[C@@H](O)CC[C@]4(C)[C@@]3([H])CC1 | ||
Formula | C21H34O3 | M.Wt | 334.5 |
Solubility | ≤25mg/ml in ethanol;25mg/ml in DMSO;25mg/ml in dimethyl formamide | Storage | Store at -20°C |
Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
Epiallopregnanolone, a endogenous 3 β-isomer of allopregnanolone, is a metabolite of progesterone. Epiallopregnanolone is a competitive antagonist at the neurosteroid site on the GABAA receptor [1]. GABAA receptors are GABA -gated chloride channels involved in mediating neuronal inhibition in the brain [2].
In vitro: Epiallopregnanolone showed no effects on the GABA-mediated chloride flux through several types of recombinant GABA receptors. Epiallopregnanolone inhibited the allopregnanolone-stimulated GABA-mediated chloride flux through GABAA receptors. Epiallopregnanolone antagonized the inhibitory effects of allopregnanolone and ethanol on the population spike in the CA1 region of the hippocampal brain slices [1]. Epiallopregnanolone selectively blocked the allopregnanolone inhibition of the population spike in the rat hippocampal CA1[3].
In vivo: In rats trained to discriminate either 0.8g/kg or 1.2 g/kg ethanol, 100 mg/kg epiallopregnanolone treatment decreased the maximum effect by 40% and 54% ethanol lever, respectively. Epiallopregnanolone significantly decreased response rates when compared with control condition [1].
References:[1] Ginsburg B C, Lamb R J. Alphaxalone and epiallopregnanolone in rats trained to discriminate ethanol[J]. Alcoholism: Clinical and Experimental Research, 2005, 29(9): 1621-1629.[2] Macdonald R L, Olsen R W. GABAA receptor channels[J]. Annual review of neuroscience, 1994, 17(1): 569-602.[3] Wang M, Bckstrm T, Landgren S. Epiallopregnanolone selectively blocks the allopregnanolone inhibition of the population spike in the rat hippocampal CA1[J]. Acta physiologica Scandinavica, 1999, 167(2): A5-A5.
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NaturalProteinStopsDeadlyHumanBrainCancerInMice
ScientistsfromJohnsHopkinsandfromtheUniversityofMilanhaveeffectivelyproventhattheycaninhibitlethalhumanbraincancersinmiceusingaproteinthatselectivelyinducespositivechangesintheactivityofcellsthatbehavelikecancerstemcells.ThereportispublishedinNature.
Themostcommontypeofbraincancer-glioblastoma-ismarkedbythepresenceofthesestem-cell-likebraincells,which,insteadoftriggeringthereplacementofdamagedcells,formcancertissue.Stemcells,unlikeallothercellsinthebody,arecapableofformingalmostanykindofcellwhentheright"signals"triggertheirdevelopment.
Fortheirtreatmentexperiment,theresearchersreliedonaclassofproteins,bonemorphogenicproteins,thatcauseneuralstem-cell-likeclusterstolosetheirstemcellproperties,whichinturnstopstheirABIlitytodivide.
Firsttheypretreatedhumanglioblastomacellswithbonemorphogenicprotein4(BMP4),theninjectedthesetreatedcellsintomousebrains.Inmiceinjectedwithcellsthatwerenotpretreated,large,invasivecancersgrew.InthemicewithBMP4-treatedcells,nocancersgrewatall.Threetofourmonthsafterinjection,allmicethatgotuntreatedcellsdied,andnearlyallmicewithBMP4-treatedcellswerealive.
Next,thescientistsdeliveredslow-releaseBMP4-containing"beads"directlyintomousebrainswithimplantedglioblastomacells.Micethatgotemptybeadsdevelopedlargemalignanttumorsanddied.MicewithBMP4beadssurvivedmuchlonger,and80percentsurvivedfourmonthsaftercancercellimplants.
"OurideaistotreatpatientswithBMP4orsomethinglikeitrightaftersurgerytoremoveglioblastomainhopesofpreventingtheregrowthofthecancerandimprovingsurvivaltime,"saysAlessandroOlivi,M.D.,directoroftheDivisionofNeurosurgicalOncologyatHopkinsandacontributortothestudy.
OlivisaysclinicalstudiesusingBMP4couldbeginwithinayearand,ifsuccessful,drugtherapiescouldbeavailabletothepublicwithinthreetofouryears.
"ThiswasproofoftheideathatBMPscouldstopglioblastomabydepletingthestem-cell-likepopulationthatfeedsit,"saysHenryBrem,M.D.,chairmanoftheDepartmentofNeurosurgeryatHopkinsandacollaboratorinthestudy."Thisopensexcitingdoorstofutureresearchintotreatmentsandtherapiesforsuchadevastatingdisease."

