CMS121

Tlhaloso e Khutšoanyane:

CMS121, mofuta o kopaneng oa fisetin, k'hemik'hale e fumanoang litholoana le meroho, mohopolo o ntlafalitsoeng, 'me e liehisa ho senyeha ha methapo mefuteng ea litoeba tsa lefu la Alzheimer's.

CMS121 ke quin oline e nkeloang sebaka e nang le tšebetso ea neuroprotective, anti-inflammatory, antioxidative, le renoprotective. E boloka maemo a glutathione (GSH) ho HT22 mouse hippocampal cell in vitro ka pel'a glutamate, e etsa hore ho be le phapang ea lisele tsa PC12, e thibela LPS-induced N9 microglial activation ka 82% ho N9 microglia, 'me e senya li-radicals tsa mahala ka har'a mahloriso a Trolox (TEAC) a lekanang le ts'ebetso ea Trolox. CMS121 e sireletsa khahlanong le ischemia le oxytosis ho li-phenotypic screens ka liseleng tsa HT22 in vitro tse nang le litekanyetso tsa EC50 tsa 7 le 200 nM bakeng sa ho thibela lefu la iodoacetic acid-kapa glutamate-induced cell, ka ho latellana. E boetse e renoprotective, e fokotsa ho lahleheloa ke boima ba liphio le ho fokotsa polelo ea TNF-α, caspase-1, le inducible nit ric oxi de synthase (iNOS) ka mohlala oa mouse oa SAMP8 oa lefu le sa foleng la liphio le amanang le ho tsofala ka potlako ha le tsamaisoa ka tekanyo ea 10 mg / kg ka letsatsi ho qala ka likhoeli tse robong.

4-(4-(cyclopentyloxy)quinolin-2-yl)benzene-1,2-diol ke motsoako o boetseng o bitsoa CMS121. Ho rarahana ha motsoako ona ho fana ka maikutlo a hore e kanna ea ba le thepa e ikhethang le ts'ebeliso e ka bang teng. Ho utloisisa bohlokoa ba eona, e thusa ho khetholla lihlopha tse sebetsang tse teng le ho sekaseka phello e ka bang teng. Ho ba teng ha reng ea quinoline ho fana ka maikutlo a hore motsoako ona o ka ba le ts'ebetso ea baeloji. Limolek'hule tse nkiloeng ho quinoline li tsejoa ka mefuta ea tsona ea tlhaho e fapaneng, ho kenyeletsoa mesebetsi ea antibacterial le anti-inflammatory. Ho khomarela sehlopha sa cyclopentyloxy ho ka kenya letsoho ho solubility ea motsoako kapa ho ntlafatsa ts'ebetso ea eona ea likokoana-hloko ka liphello tsa steric. Lithutong tsa lisele tsa HT22, CMS-121 e bonts'itse litlamorao tse kholo tsa neuroprotective, ho sireletsa lisele tsena ka katleho ho tsoa ho ischemia le tšenyo ea oxidative. Ho feta moo, CMS-121 e na le thepa ea bohlokoa e khahlanong le ho ruruha, e bontšang bokhoni ba eona ba ho fetola likarabo tsa ho ruruha. Ka ho etsa joalo, CMS-121 e na le monyetla oa ho fokotsa ho ruruha ha lisele le litho tse fapaneng. CMS-121 e na le ts'ebetso e matla ea pharmacological e le inhibitor ea acetyl-CoA carboxylase 1 (ACC1). Tšusumetso ea eona e matla ea ho thibela ACC1 e e etsa motsoako o ts'episang

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Lintlha tsa Sehlahisoa

Li-tag tsa Sehlahisoa

Lebitso la Sehlahisoa:CMS121

Lebitso le Leng:CMS-121;

1,2-Benzenediol,4--[4-(cyclopentyloxy)-2-quinolinyl]-;

4-(4-(cyclopentyloxy)quinolin-2-yl)benzene-1,2-diol(CMS121);

ACC,AcetylCoenzymeACarboxylase, lefu, neuroprotective,inhibit,anti-inflammatory,mitochondrial,Alzheimer's,antioxidative,acetylation,Inhibitor,H3K9,Acetyl-CoACarboxylase,CMS121,dementia,ACC1,CMS-121

NOMORO YA CAS:1353224-53-9

Tekanyetso: 98.0% Min

Mmala: Phofo e tshehla e kganyang

Ho paka: 25kg / DRUMS

CMS121: Phatlalatso ea Neuroprotective Compound bakeng sa Bophelo bo Botle ba Tsebo le ka Ntle ho

Selelekela
CMS121, motsoako o matla oa fisetin-flavonoid e fumanoang litholoana le meroho-e hlahile e le motsoako oa mobu o nang le melemo e mengata bakeng sa bophelo bo botle ba methapo, khahlanong le botsofali le taolo ea metabolism. E tšehelitsoe ke lipatlisiso tse batsi tsa pele ho kliniki, CMS121 e bonts'a bokhoni bo makatsang ba ho sebetsana le lefu la Alzheimer's (AD), tahlehelo ea kutlo e amanang le lilemo, le ho se sebetse hantle ho amanang le botenya.

Melemo ea Bohlokoa ea CMS121

Neuroprotection Khahlanong le Lefu la Alzheimer
CMS121 e lebisa tlhokomelo ea mafura a acid synthase (FASN), ho fokotsa lipid peroxidation-e leng mokhanni oa bohlokoa oa ho senyeha ha neuronal. Mefuteng ea litoeba tsa AD, CMS121 e khutlisitse tahlehelo ea mohopolo le ho fokotseha ha kelello, 'me litoeba tse tšoaroang li sebetsa ka mokhoa o ts'oanang le taolo e phetseng hantle litekong tsa boitšoaro. Liteko tsa bongaka li ntse li tsoela pele ho netefatsa litlamorao tsena ho batho.
Ho Boloka Kutlo e Amanang le Lilemo
CMS121 e sireletsa khahlanong le botsofali ba kutlo ho litoeba tsa SAMP8, mohlala oa bokooa ba kutlo bo amanang le lilemo (ARHI). E boloka haholo lisele tsa moriri oa kahare (IHC) synapses le ho tsitsisa menyako ea kutlo bohareng ba maqhubu (12-16 kHz), e fanang ka tšepo ea ho fokotsa tahlehelo ea kutlo "e patiloeng".
Liphello tsa Metabolic le Anti-Botenya
Lithuto tsa morao-rao li senola bokhoni ba CMS121 ba ho khutlisa botenya bo bakoang ke botsofali le ho ntlafatsa bophelo bo botle ba metabolism. Litoeba tse phekotsoeng li bonts'itse mafura a fokotsehileng, ho eketseha ha mafura, le metabolism e matlafalitsoeng ea tsoekere, e amanang le maemo a phahameng a metabolite a molemo joalo ka acetyl-CoA le butyrate.

Mekhoa ea Ts'ebetso

Thibelo ea FASN: Ka ho theola maemo a FASN, CMS121 e fokotsa lipid peroxidation le khatello ea oxidative, e sireletsang li-neuron le lisele tsa cochlear ho senya.
Ntlafatso ea Mosebetsi oa Mitochondrial: CMS121 e boloka maemo a acetyl-CoA, e tšehetsa metabolism ea matla a boko le polelo ea liphatsa tsa lefutso.
Anti-Inflammatory Properties: E hatella neuroinflammation le microglial activation, ea bohlokoa ho AD le mathata a metabolic.

Likopo le Lipatlisiso tse Tsoelang Pele
CMS121's oral bioavailability le profil ea polokeho e etsa hore e be mokhethoa ea tšepisang bakeng sa:

Thibelo ea AD le Kalafo: Ho shebana le ho fokotseha ha kelello ea pele.
Mehato ea Tahlehelo ea ho Utloa: Ho sireletsa khahlanong le ARHI ho batho ba tsofetseng.
Metabolic Syndrome Management: Ho sebetsana le botenya le ho hanyetsa insulin.

Mantsoe a sehlooho
Ho ikamahanya le mekhoa ea ho batla, litaba tsena li kopanya mantsoe a bohlokoa a bohlokoa joalo kamotsoako oa neuroprotective,Phekolo ea lefu la Alzheimer,tlatsetso e thibelang botsofali,thibelo ea tahlehelo ea kutlo, lebophelo bo botle ba metabolism.

Qetello
CMS121 e emela phetoho ea paradigm ho rarolla mathata a amanang le botsofali a methapo ea kutlo le metabolism. E tšehetsoa ke lintlha tse matla tsa preclinical le liteko tse tsoelang pele tsa kliniki, e fana ka mokhoa o akaretsang oa ho ntlafatsa boleng ba bophelo. Bakeng sa lintlha tse ling mabapi le ho fumana chelete kapa litšebelisano, ikopanye le [Lebitso la K'hamphani ea Hao], moetapele oa litharollo tse ncha tsa neurohealth.

E fetileng: J-147 Phofo

E 'ngoe: Magnesium Acetyl Taurate