China 200124-22-7 Tert-butoxycarbonyl-arginine(Pbf)-OH uMvelisi kunye neFactory |Jiayinglai

200124-22-7 Tert-butoxycarbonyl-arginine(Pbf)-OH

Inkcazelo emfutshane:

Imbonakalo	Iikristale eziMhlophe ukuya kwi-Off-White okanye umgubo wekristale.
MF	I-C24H38N4O7S
MW	526.65
Ubunyulu	98+

Thumela i-imeyile kuthi

Iinkcukacha zeMveliso

Imeko yezothutho&ecetyiswayo indlela yokuthumela ngenqanawa:
ngomoya, ngolwandle okanye nge-express

Imeko yokugcina:
Itywinwe kwindawo eyomileyo, Gcina kwisikhenkcisi, ngaphantsi kwe -20°C

Ubuncinci boMyinge woMyalelo:
Uthethathethwano

Isiqinisekiso:
COA, HPLC, GC, HNMR, Assay, Water Content(KF), TLC iyafumaneka

Izithethantonye

N5-[[[(2,3-Dihydro-2,2,4,6,7-pentamethylbenzofuran-5-yl)sulfonyl]amino]iminomethyl]-N2-BOC-L-ornithine;
I-Nα-Boc-Nω- (2,2,4,6,7-pentamethyldihydrobenzofuran-5-sufonyl) -L-arginine;
I-Nalpha-Boc-Nomega-(2,2,4,6,7-pentamethyl-2,3-dihydrobenzo[b]furan-5-sulfonyl) -L-arginine;
I-BOC-ARGININE(PBF)-OH;BOC-L-ARG(PBF)-OH;
I-BOC-N-OMEGA-(2,2,4,6,7-PENTAMETHYLDIHYDROBENZOFURAN-5-SULFONYL)-L-ARGININE

Ukupakishwa kwangaphakathi

Ngokuqhelekileyo zisetyenziselwa ukupakisha umgubo.Yaye anokuthintela ukukhanya kwelanga namanzi ukuba angabi mabi.

ukupakisha kwangaphandle

Ibhokisi elukhuni inokukhusela iimveliso zakho ekuqhekekeni kwaye zibe manzi.

Usetyenziso

I-Boc-Arg (Pbf) -OH yi-arginine derivative.
I-Bivalirudine, i-anticoagulant yokwenziwa engumzala we-20-peptide ye-hirudin, yavunywa ukuba ithengiswe e-United States ngo-2000. I-injection yinto emhlophe, ekhululekile okanye i-amorphous solid.I-Bivarudine inokubophelela ngokuthe ngqo kwindawo ye-thrombin ye-catalytic kunye ne-anion yangaphandle yokubopha indawo, kwaye inqanda ngokuthe ngqo umsebenzi we-thrombin, ngaloo ndlela inqanda ukusabela okubangelwayo kunye nokunyanzeliswa kwe-thrombin, kwaye umphumo wayo uguqulwa.I-Bivarudine isetyenziswa kakhulu njenge-anticoagulant ye-elective percutaneous coronary intervention (PCI) kubantu abadala.
I-Bivarudine yi-inhibitor ethe ngqo ye-thrombin, ebophelela ngokukodwa kwiindawo ze-catalytic kunye ne-anion exo-binding sites of thrombin free kunye ne-thrombus.Inkqubo yokubophelela phakathi kwe-bivaludine kunye ne-thrombin iyabuyiswa, kwaye i-thrombin inokubuyisela umsebenzi wokuqala webhayoloji we-thrombin ngokucotha i-enzymolysis ye-peptide bond phakathi kwe-bivaludine Arg3-Pro4.
Uphononongo lwe-in vitro lubonise ukuba i-bivarudine ayinakunqanda kuphela i-thrombin yamahhala esecaleni, kodwa iphinda ivimbele ukubopha i-thrombin ngamahlwili egazi ngaphandle kokungathathi hlangothi ngezinto ezikhutshwe ngamaplatelets.Inokwandisa ixesha leprothrombin (APTT), ixesha le-thrombin (TT), ixesha le-prothrombin (PT) kunye nexesha elisebenzayo le-coagulation (ACT) elisebenza ngeplasma eqhelekileyo.Kukho ubudlelwane bomgca kunye noxinzelelo lwe-bivarudine, kodwa ukuba olu lungelelwaniso lukhona kwisicelo seklinikhi akucaci.
Kuye kwaxelwa kwiincwadi ukuba i-pharmacokinetics yezigulane ezihamba nge-coronary angioplasty (PTCA) zihambelana emva kokulawulwa kwe-intravenous ye-bivarudine.Isigulane sanikwa i-1 mg / kg nge-intravenously njenge-dose yomthwalo, ilandelwa enye infusion ye-IV ye-2.5 mg / kg / hr kwiiyure ze-4, ezizinzile kwi-12.3 ± 1.7 mg / ml kwi-vivo.I-Bivarudine ihlanjululwa kwi-plasma nge-renal hydrolysis kunye ne-protease degradation.Ukukhutshwa kwesiqingatha-ubomi bezigulane ezinomsebenzi oqhelekileyo wezintso malunga ne-25min, kunye ne-clearance-half-life yezigulane ezinobunzima obuphakathi kunye nobunzima bokungaphumeleli kwezintso kwandiswa.Ngokumalunga ne-25% ye-bivarudine inokususwa nge-dialysis kwaye ihlanjululwe nge-hemodialysis.I-ACT kufuneka ibekwe esweni kwizigulane ezinokukhubazeka kwezintso.Kumavolontiya anempilo, umphumo we-anticoagulant wabonwa ngokukhawuleza emva kokulawulwa kwe-intravenous ye-bivarudine, kunye ne-PT ende, i-ACT kunye ne-APTT.Iyure enye ukuya kwiiyure ezimbini emva kokuhoxiswa, i-ACT ibuyele kwinqanaba lolawulo lwangaphambili.

iimveliso ezinxulumene

Cbz-Phe-Arg-OH	Boc-L-Arg-OH.HCl
Arg-Tyr-Oet	I-Boc-L-Arg-OH.HCl.H2O
HL-Arg-OH	I-Boc-D-Arg-OH•HCl•H2O
I-HD-Arg-OH	I-Boc-Arg(Cbz)-OH
I-DL-Arg-OH	Fmoc-L-Arg-OH
L-Arg-Ome.2Hcl	Fmoc-D-Arg-OH
D-Arg-Ome.2HCl	Fmoc-L-Arg(NO2)-OH
L-Arg(Pbf)-OH	Fmoc-L-Arg(Pbf)-OH
I-D-Arg (NO2)-OH / N-NO2-D-Arg	Fmoc-HoArg(Pbf)-OH
HL-Arg(NO2)-OH	Fmoc-Arg(Tos)-OH
HL-Arg (Tos)-OH	Fmoc-D-Arg(Tos)-OH
L-Arg-NH2	Fmoc-D-Arg(Pbf)-OH
Boc-L-Arg-OH	Cbz-Arg-OH
I-Boc-D-Arg(Pbf)	Cbz-D-Arg-OH
Boc-Arg-Oet	Cbz-L-Arg(Pbf)-OH
Boc-L-Arg-Ome	Cbz-D-Arg(pbf).CHA
Boc-L-Arg(Tos)-OH	Cbz-D-Arg-Gly-OH
I-Boc-L-Arg(NO2)-OH	L-Arg(Pbf)-Asp
Fmoc-L-HomoArg-OH	L-Homoarg.hcl

Ukongama

1. Inkonzo yeR&D iyafumaneka
2. Umvelisi oqinisekisiweyo we-ISO, isiqinisekiso somgangatho
I-3.Ikhosi epheleleyo yenkonzo yokulandelela ngexesha lemveliso
4.Ixabiso eliphezulu elisebenzayo
5.Amaxwebhu esiqinisekiso somgangatho anikwe ngokwesicelo somthengi
I-6.Inkonzo enkulu emva kokuthengisa, ukugcina ubudlelwane obusondeleyo kunye nomthengi
I-7.Isixhobo esipheleleyo sokunceda ukunciphisa iindleko zokuthumela ngenqanawa
I-8.Isampuli yamahhala enikezelwa ukujonga umgangatho ngaphambi kwayo nayiphi na intlawulo
9.Ixesha lentlawulo ekuxoxwe ngalo
Abathengi be-10.Assit bajongana nemicimbi yaseTshayina