TMC207 CAS 843663-66-1 Pure >99.5% (HPLC)
Ingoa matū | TMC207 |
Nga kupu taurite | 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 |
Tau CAS | 843663-66-1 |
Tau CAT | RF2336 |
Tūnga Taonga | I roto i te Stock, Production Tauine Up ki Taranata |
Tātai rāpoi | C32H31BrN2O2 |
Taumaha rāpoi | 555.516 |
Iwi Whakarewa | 104℃ |
Kiato | 1.322±0.06 g/cm3 |
Tairongo | Hygroscopic.Maamaa, Maamaa Maama |
Waitohu | Ruifu Chemical |
Tūemi | Whakatakotoranga |
Te ahua | Paura Ma, Paura-Ma ranei |
Te Maama / Tikanga Tatauria | >99.5% (HPLC) |
Ngaronga i te whakamaroke | <0.50% |
Te toenga i runga i te mura | <0.20% |
Te poke takitahi | <0.10% |
Isomer | <0.10% |
Nga poke katoa | <0.50% |
Konga Taamaha (hei Pb) | <20ppm |
Arsenic (As) | <2.0ppm |
Spectrum Infrared | He rite ki te Hanganga |
Proton NMR Spectrum | He rite ki te Hanganga |
Paerewa Whakamatau | Paerewa hinonga |
Whakamahinga | API |
Mōkī: Pounamu, Peeke konumohe konumohe, 25kg / Kaata Drum, kia rite ranei ki te hiahia a te kaihoko
Tikanga Rokiroki:Whakaorangia i roto i nga ipu kua hiri ki te waahi makariri me te maroke;Tiaki i te marama me te makuku
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(CAS: 843663-66-1), (e mohiotia ana ko TMC207 me R207910), he mea hokohoko i raro i te ingoa hokohoko Sirturo, he rongoa rongoa antimycobacterial diarylquinoline e pa ana ki te mate kohi ma te aukati i te mahi a te M. tuberculosis ATP synthase proton pump.Ko te whakahiato ATP o te mycobacteria he hua antibacterial me te huakita.I whakamahia ma te haumanu ki te rongoa i te mate kohi pakeke-atete ki nga rongoa maha (MDR-PTB).He rite tonu te mahi huakita a TMC207 ki nga riaka tairongo M. tuberculosis me nga riaka atete, a he pai hoki te whakamaaramatanga ki nga huakita moe.I te Hakihea 2012, i whakaaetia e te US FDA te TMC207 hei waahanga o te rongoa whakakotahi mo te maimoatanga o te mate kohi aatete ki nga rongoa maha (MDRTB).Ko TMC207 te rongoa tuatahi kua whakamanahia mo te MDR-TB, a ko te whakaaetanga tuatahi mai i tetahi karaehe hou o nga rongoa mate kohi i roto i nga tau 40 kua hipa.Na te nui o te hiahia mo te rongoa MDR-TB, i tukuna e te FDA te whakaaetanga tere a TMC207 i runga i nga hua o te Wāhanga II, kia uru atu nga turoro ki te rongoa i te wa e mahia ana etahi atu rangahau haumanu.Ko te TMC207 he diarylquinoline i kitea mai i te rautaki tirotiro-a-tinana-katoa me te Mycobacterium smegmatis i whakamahia hei whakakapi mo M. tuberculosis.Ko TMC207 he enantiomer kotahi o te tukitukitanga tuatahi.He kaha te mahi a TMC207 ki te mycobacteria, a he kaha ki te mate kohi M. tuberculosis-tairongo me te aukati tarukino.Ko te tikanga o te mahi a TMC207 he mea ahurei i waenga i nga raau taero anti-TB me te aukati i te synthase ATP mycobacterial;kare i te kaha ki te ATP synthase tangata.He mahi in vivo a TMC207 i roto i te maha o nga tauira preclinical o te mate TB, ko ia anake me te hono tahi me etahi atu apiha anti-TB, a he mahi huakita i roto i nga tauira mate TB kua whakapumautia.Ka whakahiatotia a TMC207 i roto i nga kaupae e rima mai i te 3-Phenylpropionic Acid me te para-Bromoaniline.I muri i te hanganga o te amide, ko te maimoatanga me te POCl3 me te DMF i raro i nga tikanga Vilsmeier-Hack i hoatu he hua 2-Chloroquinoline.Ko te maimoatanga me te konutai methoxide, ka whai i te whakamaaramatanga me te 3-(Dimethylamino)-1-(naphthalen-1-yl)propan-1-one, me te wehenga o nga isomer i homai TMC207.