TMC207 CAS 843663-66-1 Mimọ>99.5% (HPLC)

Apejuwe kukuru:

Orukọ: TMC207

Synonyms: R207910

CAS: 843663-66-1

Mimọ:> 99.5% (HPLC)

Irisi: Funfun tabi Paa-White Powder

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Kemikali Properties:

Orukọ Kemikali TMC207
Awọn itumọ ọrọ sisọ TMC-207, R207910;Sirturo;(αS, βR) -6-Bromo-α- [2- (dimethylamino) ethyl] -2-methoxy-α-1-naphthalenyl-β-phenyl-3-Quinolineethanol;1- (6-Bromo-2-methoxyquinolin-3-yl) -4-dimethylamino-1-phenyl-2- (1-naphthyl) 2-butanol
Nọmba CAS 843663-66-1
NỌMBA CAT RF2336
Iṣura Ipo Ninu Iṣura, Iwọn iṣelọpọ Ti o to Awọn Toonu
Fọọmu Molecular C32H31BrN2O2
Òṣuwọn Molikula 555.516
Ojuami Iyo 104℃
iwuwo 1.322 ± 0,06 g / cm3
Ni imọlara Hygroscopic.Imọlẹ Imọlẹ, Afẹfẹ Ifamọ
Brand Ruifu Kemikali

Awọn pato:

Nkan Awọn pato
Ifarahan Funfun tabi Pa-White Powder
Mimọ / Analysis Ọna > 99.5% (HPLC)
Pipadanu lori Gbigbe <0.50%
Aloku lori Iginisonu <0.20%
Eyikeyi Olukuluku aimọ <0.10%
Isomer <0.10%
Lapapọ Awọn Aimọ <0.50%
Awọn irin Heavy (gẹgẹbi Pb) <20ppm
Arsenic (Bi) <2.0ppm
Infurarẹẹdi julọ.Oniranran Ni ibamu si Eto
Proton NMR julọ.Oniranran Ni ibamu si Eto
Igbeyewo Standard Standard Enterprise
Lilo API

Package & Ibi ipamọ:

Package: Igo, apo bankanje aluminiomu, 25kg / Paali ilu, tabi gẹgẹ bi ibeere alabara

Ipò Ìpamọ́:Fipamọ sinu awọn apoti ti a fi edidi ni itura ati ibi gbigbẹ;Dabobo lati ina ati ọrinrin

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Ohun elo:

(CAS: 843663-66-1), (ti a mọ ni TMC207 ati R207910), ti a ta labẹ orukọ iṣowo Sirturo, jẹ aramada diarylquinoline antimycobacterial oogun ti o ni ipa lori iko nipa didi iṣẹ ṣiṣe ti M. tuberculosis ATP synthase proton pump.Iṣọkan ATP ti mycobacteria ṣe ipa antibacterial ati awọn ipakokoro.Ti a lo ni ile-iwosan lati ṣe itọju iko-ara ti ko ni oogun pupọ (MDR-PTB).TMC207 ni o ni kanna bactericidal aṣayan iṣẹ-ṣiṣe lodi si M. iko kókó igara ati sooro igara, ati ki o tun ni o dara sterilization ipa lori dormant kokoro arun.Ni Oṣu Kejila ọdun 2012, US FDA fọwọsi TMC207 gẹgẹ bi apakan ti itọju apapọ fun itọju ti iko-ara ti o ni oogun pupọ (MDRTB).TMC207 jẹ oogun akọkọ ti a fọwọsi fun MDR-TB ati pe o jẹ ifọwọsi akọkọ lati ọdọ kilasi tuntun ti awọn aṣoju antituberculosis ni ọdun 40 sẹhin.Nitori iwulo aini iṣoogun giga fun atọju MDR-TB, FDA funni ni ifọwọsi isare TMC207 ti o da lori awọn abajade Ipele II, pese awọn alaisan ni iwọle si oogun lakoko awọn iwadii ile-iwosan ni afikun.TMC207 jẹ diarylquinoline ti a ṣe awari lati ọna-giga, ilana ibojuwo gbogbo-cell pẹlu Mycobacterium smegmatis ti a lo bi aropo fun M. iko.TMC207 jẹ enantiomer kan ti kọlu iboju akọkọ.TMC207 ni o ni agbara ati aṣayan aṣayan iṣẹ-ṣiṣe lodi si mycobacteria, ati ki o jẹ lọwọ lodi si awọn oogun-kókó ati oògùn-sooro M. iko.Ilana iṣe ti TMC207 jẹ alailẹgbẹ laarin awọn oogun egboogi-TB ati pe o kan idinamọ ti mycobacterial ATP synthase;ko ṣiṣẹ lodi si ATP synthase eniyan.TMC207 ni iṣẹ-ṣiṣe ni vivo ni ọpọlọpọ awọn awoṣe preclinical ti ikolu TB, nikan ati ni apapo pẹlu awọn aṣoju egboogi-TB miiran, ati pe o ni iṣẹ-ṣiṣe kokoro-arun ni awọn awoṣe ikolu TB ti iṣeto.TMC207 jẹ iṣelọpọ ni awọn igbesẹ marun lati 3-Phenylpropionic Acid ati para-Bromoaniline.Ni atẹle idasile amide, itọju pẹlu POCl3 ati DMF labẹ awọn ipo Vilsmeier-Hack fun ọja 2-Chloroquinoline kan.Itọju pẹlu iṣuu soda methoxide, ti o tẹle pẹlu condensation pẹlu 3- (Dimethylamino) -1- (naphthalen-1-yl) propan-1-one, ati iyapa awọn isomers fun TMC207.

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