Re fana ka 5- Azacytidine API

Re motlotlo ho fana 5- Azacytidine API, motsoako oa meriana oa boleng bo holimo o sebelisoang e le antineoplastic le antiviral agent. API ena e sebelisoa haholo kalafong ea acute myeloid leukemia, myelodysplastic pattern, le tloaelo ea myelomonocytic leukemia. Sehlahisoa sa rona se etsoa ho latela litloaelo tse tiileng tsa boleng, ho hlohlelletsa bohloeki le katleho ea sona. E fumaneha ka boholo ba liphutheloana tse mebala-bala ho lumellana le maemo a hau a khethehileng. Re tšepe hore re tla u fa matla a ka tšeptjoang le a sebetsang a 5- Azacytidine. buisana le rona motsotso ho ithuta ho eketsehileng ka sehlahisoa sena le hore na re ka u thusa joang.

Azacytidine ke eng?

5- Azacytidine phofo, e tsejoang hape e le Azacitidine kapa 5- AC, ke ntho ea lik'hemik'hale. Ke nucleoside analoge e entsoeng ka setsi sa adenine mme patch e bōpehileng joaloka selikalikoe e khethileng nitrogen heterocycle e nang le naetrojene. Ke thepa ea DNA methyltransferase 'me e lula e sebelisoa ho phekola myelodysplastic pattern(MDS), boemo ba mali.Lebitso la eona la lik'hemik'hale ke 4- Amino- 1-(- D- ribofuranosyl)(1H)- e le' ngoe, 'me nomoro ea eona ea CAS ke 320-67-2. Foromo ea eona ea lik'hemik'hale ke C8H12N4O5, 'me boima ba eona ba molek'hule ke 244.2 g/ spook. E ka fetola polelo ea liphatsa tsa lefutso mme ea ba le melemo ea tokiso maemong a kang myelodysplastic pattern(MDS) ka ho ts'oara ts'ebetso ea DNA methylation. Ka ho thibela liphetoho tsa DNA methylation, e khothalletsa kholo ea lisele tse phetseng hantle tsa hematopoietic le ho khutlisetsa morao sebopeho sa lisele tse sa phethahalang tsa hematopoietic.

Ho sibolloa ha 5-Azacytidine ho sibolloa ho qalile ka bo-1950. Kakaretso ea liphetho tsa eona e ka fumanoa mona:

Ea pele Azacytidine API pherekano e ile ea etsoa ka 1958 ke baetsi ba liteko ba tsoang Karolong ea Ntlafatso ea Lik'hemik'hale ea Mekhatlo ea Sechaba ea Bophelo bo Botle United States. Ba ile ba theha hore ntho ena e thibela methylation ea DNA ea cellular.

Setsi sa Sechaba sa Kankere (NCI) sa United States se qalile ho etsa lipatlisiso tse ncha ho azacytidine a 1964.

Azacitidine phofo e fetisitse lipatlisiso le nts'etsopele e ncha lilemong tse mashome tse fetileng. US Food and Drug Administration (FDA) e file Azacytidine (hape e boetse e bitsoa Vidaza) tlhohonolofatso ka 1985 bakeng sa ts'ebetso ea myelodysplastic pattern (MDS) e kotsi haholo. Ka lebaka leo, e 'nile ea sebelisoa kamehla ho phekola MDS hape.

Information Basic

Lebitso la Sehlahisoa: 5-Azacytidine
CAS:320-67-2
MF:C8H12N4O5
MW: 244.2
EINECS: 206-280-2
Nomoro ea MDL: MFCD00006539
Bohloeki: 99%
Botsitso: E tsitsitse lilemo tse 2
solubility: Ho qhibiliha ho DMSO (ho fihlela ho 25 mg / ml), kapa ka Metsing (ho fihlela ho 12 mg / ml).
Kopo: Kereiti ea bongaka kapa e sebelisetsoang lipatlisiso.
Packing: Ho ea ka kopo ea hau
Storage: Mocheso oa kamore.
Mokhoa o raliloeng:

Sebaka se qhibilihang: 226 ho isa ho 232 ℃

Sebaka se belang: 534.5 ℃

Ho qhibiliha ha metsi: ho qhibiliha

Boima: 2.08 g/cm ³

Sebaka sa Flash: 277 ℃

Tekanyetso ea boleng

Ho paka: 500g / mokotla; 1kg / mokotla

Maemo a polokelo: -20 ℃, bopaki ba mongobo, bo tiisitsoeng, le bopaki bo bobebe

Maemo a lipalangoang: 2-8 ℃ lipalangoang

Sehlopha: Lintho tse chefo

Karohano ea chefo: e chefo haholo

Chefo e matla: Oral LD50 ka litoeba: 572 mg / kg; Toeba ea lesapo la mpa LD50: 68 mg/kg

Litšobotsi tsa kotsi ea ho chesa: ho chesa; Ho chesa ho hlahisa mosi o chefo oa nitrogen oxide; Litla-morao tsa meriana ho bakuli: ho nyekeloa ke pelo, ho hlatsa, letšollo, le ho fokotseha ha lisele tse tšoeu tsa mali

Moemeli oa ho tima: phofo e omileng, foam, lehlabathe, carbon dioxide, metsi a atomized

ke seo kopo ea 5-Azacytidine phofo ?

Tse latelang ke litšebeliso tse ka sehloohong bakeng sa 5-Azacytidine phofo le libaka tsa ts'ebeliso ea eona:

1.Lithethefatsi tse thibelang metabolism

Pontšo e kholo ke acute myeloid leukemia e sa sebetseng khahlano le kalafo e tloaelehileng. E boetse e sebelisoa bakeng sa kankere ea matsoele, melanoma, kankere ea mala, joalo-joalo Lipontšo tse ka sehloohong tsa chefo ke leukopenia, thrombocytopenia le phokolo ea mali. Ho nyekeloa ke pelo le ho hlatsa ke litlamorao tse tloaelehileng, tse ka ntlafatsoang ka ho tšeloa nako e telele kapa ka ho sebelisa li-antiemetics lihora tse 24 ho isa ho tse 48 pele ho kalafo. Litlamorao tse ling tse chefo li kenyelletsa letšollo, mafu a neuromuscular, feberu, hypotension le lekhopho. Sehlahisoa se lokiselitsoe ka lihora tse 3-4 pele se sebelisoa.

2.A inhibitor e matla ea ho hōla le moemeli oa cytotoxic

Thibelo ea DNChemicalbookA methyltransferase, mokhoa oa bohlokoa oa taolo bakeng sa polelo ea liphatsa tsa lefutso, ho kenya tšebetsong le ho khutsisa; Lithethefatsi tsa mofets'e tse nang le ts'ebetso e fokolang ea li-antibody (Gram positive); E sebelisetsoa ho ithuta phello ea DNA e kopanyang limolek'hule nakong ea ts'ebetso ea DNA methylation

3. Ntho e ka 'nang ea e-ba le thibelo ea ho hōla le cytotoxic carrier

Ho thibela DNA methyltransferase, e leng mokhoa oa bohlokoa oa taolo bakeng sa polelo ea liphatsa tsa lefutso, tlhahiso ea liphatsa tsa lefutso, le ho thibela liphatsa tsa lefutso. Ntho ena e baka DNA demethylation kapa semi demethylation, e lumellang lintlha tse ngotsoeng ho tlama DNA le ho tsosolosa liphatsa tsa lefutso tsa tumor suppressor.

Lintlha tsa ts'ireletso

Leibole ea thepa e kotsi: T

Khoutu ea sehlopha sa kotsi: 45-46-22

Safety instructions: 53-22-36/37/39-45

WGK Jeremane: 3

Nomoro ea RTECS: XZ3017500

F: 10-23

Khoutu ea moetlo: 29349990

Lintlha tsa Lintho Tse Chefo: 320-67-2

Chefo: LD50 ka litoeba (mg / kg): 115.9 ip; 572.3 Ka Molomo (Palm, Kensler)

Pharmacological action

Azacytidine e na le phello ea eona e khahlanong le hlahala ka ho fokotsa DNA methylation le ho sebelisa cytotoxicity e tobileng mokong oa lisele tse sa tloaelehang tsa hematopoietic. Liphuputso tsa in vitro li bonts'itse hore khatello ea sehlahisoa sena ka ho thibela DNA methylation ha e sitise DNA synthesis haholo. Ketsahalo ea methylation e tlaase e ka tsosolosa mosebetsi o tloaelehileng oa liphatsa tsa lefutso tse amanang haufi-ufi le ho arohana le ho ata ha libuka tse ntle tsa lik'hemik'hale. Phello ea cytotoxic ea sehlahisoa sena e ka baka lefu la lisele tse ntseng li ata ka potlako, ho kenyelletsa le lisele tsa mofetše tse lahlileng taolo e tloaelehileng ea mochini, athe lisele tse sa atang li batla li sa tsotelle sehlahisoa sena. Kakaretso, thepa ea physicochemical, mekhoa ea ho itokisa, litlamorao tsa pharmacological, le ts'ebeliso ea azacitidine

Melemo ea Rōna

Phihlelo e ruileng: re na le Lilemo tse 13 tsa boiphihlelo ba litsebi;

Bareki lefatšeng ka bophara: rekisetsa linaha tse fetang 100;

Fana ka lihlahisoa tse fapa-fapaneng: lihlahisoa li sebelisitsoe ho mefuta eohle e meholo ea machaba lefapheng la lithethefatsi, lijo tsa lijo, litlolo, phepo ea liphoofolo le lijo tse sebetsang hantle.

Theko esale pele: MOQ e tlase ka theko ea tlholisano;

Setifikeiti sa boleng: ISO; Halal; Kosher e netefalitsoe

Tšebeletso ea ka mor'a thekiso: Sehlopha sa litsebi lihora tse 7 * 24 tšebeletso ea bareki.

Ka kakaretso, joalo ka setsebi Azacitidine API moetsi, re na le thekenoloji e tsoetseng pele, melemo e mengata, boleng bo holimo, boiphihlelo bo bongata ba tlhahiso, le lits'ebeletso tse ntle haholo. Melemo ena e tla etsa hore e hlahelle tlholisanong ea 'maraka le ho hapa tšepo le tšehetso ea bareki.

lintlha tsa rona tsa ho ikopanya: 

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