Ganaplacide-hydrochloride-KAF156-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEGanaplacidehydrochlorideCat.No.:HY-108024ASynonyms:KAF156hydrochloride;GNF156hydrochloride分?式:C??H??ClF?N?O分?量:447.91作?靶點(diǎn):Parasite作?通路:Anti-infection儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCOA.溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(223.26mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2326mL11.1630mL22.3259mL5mM0.4465mL2.2326mL4.4652mL10mM0.2233mL1.1163mL2.2326mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案，配制前請(qǐng)先配制澄的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.58mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.58mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.58mM);ClearsolutionBIOLOGICALACTIVITY1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE?物活性Ganaplacide(KAF156)hydrochloride?種?創(chuàng)的具有?服活性的咪唑哌嗪類抗瘧藥(antimalarial)。Ganaplacidehydrochloride對(duì)多種瘧原?有活性，包括耐藥寄??。Ganaplacidehydrochloride對(duì)?性和有性?液階段以及肝臟階段都有殺?作?。體外研究Ganaplacide(KAF156)hydrochlorideshowsbloodschizonticidalactivitywith50%inhibitoryconcentrationsof6to17.4nMagainstP.falciparumdrug-sensitiveanddrug-resistantstrains[1].體內(nèi)研究KAF156displayscidalactivityagainstmaturePlasmodiumfalciparumgametocytesandthusblocksparasitetransmissiontoAnophelesmosquitoes[1].Ganaplacide(KAF156)hydrochloride(1-15mg/kg;p.o.)isfullyprotectiveinacausalprophylacticmousemodelofmalaria[1].AnimalModel:Mice(causalprophylacticrodentmalariamodel)[1]Dosage:1-15mg/kgAdministration:P.o.Result:Asingleoraldoseof10mgofKAF156/kgadministered2hbeforeinfectionwasfullyprotective.REFERENCES[1].KuhenKL,etal.KAF156isanantimalarialclinicalcandidatewithpotentialforuseinprophylaxis,treatment,andpreventionofdiseasetransmission.AntimicrobAgentsChemother.2014;58(9):5060-5067.[2].LeongFJ,etal.Afirst-in-humanrandomized,double-blind,placebo-controlled,single-andmultiple-ascendingoraldosestudyofnovelImidazolopiperazineKAF156toassessitssafety,tolerability,andpharmacokineticsinhealthyadultvolunteers.AntimicrobAgentsChemother.2014;58(11):6437-6443.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Fo