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Everylotistried&testedinarelevantBIOLOGicalassay.
OurBioassay
- Hess,P. etal. (1984) Nature 311, 538.
- Nowycky,M.C. etal. (1985) Proc.Natl.Acad.Sci.U.S.A. 82, 2178.
- Bechem,M.andHoffmann,H. (1993) PflugersArch. 424, 343.
- Triggle,D.J.andRampe,D. (1989) TrendsPharmacol.Sci. 10, 507.
- Avdonin,V. etal. (1997) J.Gen.Physiol. 109, 169.
- AlomoneLabs(±)-BayK8644increasesL-typeCa2+ currentsexpressedin Xenopus oocytes.Left:I-Vrelationbefore(squares)andduring(circles)bathperfusionof5μM (±)-BayK8644 (#B-350).Right:Anexampleofcurrentresponseto200msdepolarizationto+20mV(fromholdingpotentialof-100mV)before(black)andduring(pink)perfusionof(±)-BayK8644.AlomoneLabs(±)-BayK8644modulatesthephosphorylationofERK1/2MAPKinJurkatTcells.CellswerepreincubatedwithorwithoutEGTAorNifedipinefor20minthenstimulatedwith (±)-BayK8644 (#B-350)orwith Ionomycin for10min.Thecellproteinswereblottedandprobedwithanti-phosphoERK1/2(upperpanel)orwithanti-ERK1/2(lowerpanel).
- 1.Hess,P. etal. (1984) Nature 311, 538.
- 2.Nowycky,M.C. etal. (1985) Proc.Natl.Acad.Sci. U.S.A. 82, 2178.
- 3.Bechem,M.andHoffmann,H. (1993) PflugersArch. 424, 343.
(±)-BayK8644isanopenerofallL-typechannels(CaV1family).Inthepresenceofthisagonist,channelstendtoopenforlongerperiodscausingalargeincreaseinthechannelmacroscopicresponse.
Thenetactivityoftheracemicmixisthatofthe(-)-enantiomeragonisticactivity.
(±)-BayK8644isawidelyusedL-typeCa2+channelactivatorinvariousneuronal,muscle,endocrine,thyroidandothercelltypes.1-3
(±)-BayK8644(#B-350)isahighlypure,synthetic,andbiologicallyactivecompound.