Exenatide acetatese yon dwòg peptides ki se yon blan pou poud blan blan ak prèske pa gen okenn odè . molekilè fòmil C186H286N50O62s, CAS 141732-76-5. soluble nan Solvans òganik tankou dlo, methanol, ak DMSO {{6} Fòm . Nan tanperati chanm, li se relativman ki estab . Sepandan, tanperati ki wo ka afekte estabilite li yo ak mennen nan dekonpozisyon . Se poutèt sa, li nesesè nan magazen ak transpò pwodwi anba kondisyon ki apwopriye ak imidite {{10} Dyabèt .
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Customized boutèy boutèy ak bouchon:
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Exenatide acetate gen yon varyete de aplikasyon pou, sitou konsantre nan jaden yo nan tretman dyabèt ak rechèch byomedikal . Sa ki anba la a se yon entwodiksyon espesifik:
Tretman dyabèt
Ipoglisemi mekanis
Exenatide acetate is a glucagon-like peptide-1 (GLP-1) analogue. By simulating the physiological effects of GLP-1, it promotes glucose-dependent insulin secretion, inhibits inappropriate glucagon secretion, slows down gastric emptying, thereby improving the Sansiblite nan tisi periferik ensilin ak akonplisman efè a nan bese sik nan san .
Aplikasyon nan klinik
Li se apwopriye pou tip 2 pasyan dyabetik ki gen glikoz nan san pa byen kontwole malgre itilize nan metformin pou kont li, sulfonylureas, oswa konbinezon an nan metformin ak sulfonyLureas . etid yo montre ke ègzenates ka diminye jèn ak postprandyal konsantrasyon glikoz nan pasyan ki gen dyaboz ki gen pou amelyore nan pasyan ki gen pou amelyore aktive nan pasyan ki gen 2 kazasyon ak amelyore nan pasyan ki gen pou jwenn akerie nan pasyan ki gen 2 kazite ki gen pou amelyore nan pasyan ki gen 2 kazasyon ki gen kalite aktive ak amelyore nan pasyan ki gen 2 kazo ki gen 2 kazo ki gen 2 ka amelyore ak amelyore nan pasyan yo ki gen yon ti jan ki gen yon ti jan ki gen pou amelyore nan pasyan ki gen yon ti jan ki gen 2 an.
Karakteristik famasi
Sekresyon ensilin glikoz-depandan
Li sèlman ki lakòz ensilin lage lè konsantrasyon glikoz leve . Lè konsantrasyon glikoz nan san gout ak apwòch nivo nòmal, sekresyon ensilin diminye, kidonk diminye risk pou yo ipoglisemi .
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Restore premye-faz repons lan ensilin
Pasyan ki gen dyabèt tip 2 tipikman manke premye-faz repons lan ensilin (se yon gwo kantite ensilin sekrete nan lespas 10 minit apre piki nan venn glikoz) . exenatide asetat ka retabli repons sa a ak amelyore reyaksyon nan selil pankreyas nan glikoz .}}
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Diminye sekresyon glikagon
Pandan ipèglisemi, diminye sekresyon glikagon, pi ba konsantrasyon glikagon serom, diminye pwodiksyon glikoz epatik, diminye demann ensilin, ak nan menm tan an, pa domaje repons lan glikagon nòmal nan ipoglisemi .}
03
Ralanti gastric vide
Ralanti desann pousantaj la nan ki glikoz soti nan manje antre nan sikilasyon an ede estabilize fluctuations sik nan san .
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Rechèch byomedikal
Etid obligatwa reseptè:Acetate exenatide, kòm yon konpoze polipeptid, ka mare nan reseptè espesifik ak se apwopriye pou rechèch molekilè famasi . pa etidye karakteristik obligatwa li yo ak reseptè sib, yon moun ka jwenn yon konpreyansyon an pwofondè nan mekanis li yo nan aksyon ak siyal transduction chemen .}}
Byolojik D '
Cy 5- Exenatide acetate: yon derive exenatide ki make ak Cy5 lank fluorescent, apwopriye pou rechèch biomolekilè, analiz reseptè obligatwa ak eksperyans bioimaging . karakteristik yo ki gen apeprè 64 nm, excitation winthe0 nm, Emisyon Wouzin yo te gen rapò ak {2}. Rapò siyal-a-bri ak entèferans ki ba background nan mikroskopi fluoresans, sitometri koule ak nan eksperyans D 'vivo .
Jaden Aplikasyon: Li se apwopriye pou konfokal mikroskopi fluoresans, fluoresans-aktive klasman selil (FACS), ak fluoresans sonorite transfè enèji (FRET) eksperyans, epi yo ka itilize yo etidye distribisyon an nan exenatide nan selil, entèraksyon reseptè, ak pwosesis metabolik .}}
Rechèch absorption selil:Etidye absorption ak distribisyon exenatid nan diferan kalite selil se itil pou konprann karakteristik farmakokinetik li yo ak mekanis nan aksyon nan vivo .
Rechèch farmakokinetik
Fluorescent ki make dérivés de exenatide acetate (tankou cy 5- exenatide acetate) ka itilize pou etidye distribisyon li yo ak pwosesis metabolik nan vivo, bay yon baz enpòtan pou rechèch dwòg ak devlopman ak optimize .
Exenatide acetateÈske gen yon pakèt itilizasyon ak enplike nan anpil aspè, se konsa ki jan yo amelyore efikasite sentèz li yo te vin yon enkyetid pou chèchè anpil . Nan tèks sa a, nou pral prezante yon wout sentetik ki te pwopoze pa chèchè nou yo .
Etap 1: Sentèz Fmoc Gly Pro SE (TBU) SE (TBU) Gly Ala Pro Pro Se (TBU) - MBHA RESIN
1) sentèz FMOC SER (TBU) - MBHA résine
After swelling Fmoc Rink Amide MBHA Resin with N, N-dimethylformamide, remove Fmoc twice with a mixture of piperidine and N, N-dimethylformamide in a volume ratio of 1:4. Add N, N-dimethylformamide, Fmoc Ser (tBu) - OH, 1- Hydroxyphenylpropanetriazole, benzotriazole -n, n, n ', n' - tetramethylurea tetrafluoroboric asid, n, n ' - diisopropylethylamine, ak brase nan tanperati a pou {{{{ Mbha résine .
2) sentèz FMOC Pro SE (TBU) - MBHA résine
FMOC SER (TBU)-MBHA résine te retire de fwa lè l sèvi avèk yon melanj de piperidine ak N, N-dimethylformamide nan yon rapò volim nan 1: . N, N-dimethylformamide, FMOC Pro, 1- hydroxyhenylpropoplopopoplopop- N ' - tetramethylurea tetrafluoroboric asid, n, n' - diisopropylethylamine te ajoute, ak tèt nan tanperati chanm pou 1-3 èdtan anba pwoteksyon nitwojèn jwenn fmoc pro ser (tbu) - mbha rezin .
3) Sentèz FMOC Gly Pro SE (TBU) SE (TBU) Gly Ala Pro Pro SE (TBU) - MBHA résine
Konekte FMOC Pro OH, FMOC Pro OH, FMOC ALA OH, FMOC Gly OH, FMOC SER (TBU) OH, FMOC SER (TBU) OH, FMOC Pro OH, ak FMOC GLY OH POU FMOC PRO SE (TBU) SE (TBU) - (TBU) - gly ala pro se (TBU) - MBHA résine .
Etap 2: Sentèz FMOC Lys (BOC) - ASN (TRT) - Gly COOH
1) sentèz FMOC gly -2- CTC résine
Apre anfle 2- chlorotrityl klori résine ak dichloromethane, ajoute dichloromethane, fmoc gly-oh, n, n '- diisopropylethylamine, ak brase nan tanperati chanm pou {{}}}} résine .
2) sentèz nan FMOC Lys (BOC) - ASN (TRT) - Gly -2- CTC résine
Apre metòd la nan Etap 1 (2), konekte FMOC ASN (TRT) - OH ak FMOC Lys (BOC) - O sekans nan FMOC Gly -2- CTC résine pou jwenn FMOC Lys (Boc) - ASN (TRT) - Gly -2- resin CTC {{{{
3) Tretman koupe
Add Koupe likid nan FMOC Lys (BOC) - ASN (TRT) - Gly -2- CTC résine, brase nan tanperati chanm pou 1-3 èdtan, filtre, ajoute filtraj la etè frèt, presipite, ak FMOC Lys (BOC) - ASN (TRT) - GNE COOTH / / 6 / / / asid trifluoroacetic ak dichloromethane nan yon rapò volim nan 1:99 oswa 2:98, oswa yon melanj de trifluoroethanol ak asid acetic ak dichloromethane nan yon rapò volim nan 2: 1: 7.}
Etap 3: Sentèz FMOC Val Arg (PBF) - Leu Ile Glu a (OTBU) - TRP Leu COOH
Apre metòd la nan etap 2 (1), konekte FMOC Leu OH a 2- chlorotrityl klori a résine jwenn fmoc leu 2- CTC résine . Lè sa a ,, Phe OH, FMOC Leu OH, FMOC Arg (PBF) OH, FOMC Val Arg (PBF) - Leu Li Ile Glu (OTBU) - TRP Leu -2- CTC Résine, FMOC Val Arg (PBF) - Leu Ile Glu (Otc) - TRPE. (3) Pou jwenn FMOC Val Arg (PBF) - Leu Ile Glu a (OTBU) - TRP Leu COOH .
Etap 4: Sentèz FMOC te rankontre Glu (OTBU) - Glu (OTBU) - Glu (OTBU) - ALA COOH
Following the method in step 2 (1), connect Fomc Ala-OH to the 2-chlorotrityl chloride resin to obtain Fmoc Ala-2-CTC resin. Then, follow the method in step 2 (2) to connect Fomc Glu (otBu) - OH, Fmoc Glu (otBu) - OH, Fmoc Glu (otBu) - OH, Fomc Met Glu (otBu) - Glu (otBu) - Glu (otBu) - Glu (otBu) - A la-2-CTC Resin, Fmoc Met Glu (otBu) - Glu (otBu) - Glu (otBu) - Ala-2-CTC Resin was cut according Nan metòd la nan etap 2 (3) jwenn FMOC te rankontre Glu (OTBU) - Glu (OTBU) - Glu (OTBU) - Ala -COOH .
Etap 5: Sentèz FMOC THR (TBU) - SE (TBU) - ASP (OTBU) - Leu SE (TBU) - Lys (BOC) - GLN (TRT) - COOH
Apre metòd la nan etap 2 (1), konekte FOMC Gln (TRT) - OH nan 2- chlorotrityl klori résine a jwenn FMOC Gln (TRT) {{4} CTC résine . OH, FMOC Leu OH, FMOC ASP (OTBU) - O, FMOC SER (TBU) - OH, FOMC THR (TBU) - OH) nan FMOC GLN (TRT) {{13} CTC résine {{14} (TBU) - Lys (BOC) - Gln (TRT) -2- CTC résine, FMOC THR (TBU) - Ser (TBU) - Asp (OTBU) - Leu Ser (TBU) - LYS (BOC) - GLN (TRT) {{ jwenn fmoc thr (tbu) - ser (tbu) - asp (otbu) - leu ser (tbu) -2- ctc résine . - lys (Boc) -gln (trt) -COOH .}
Etap 6: Sentèz FMOC li (TRT) Gly Glu (OTBU) Gly Thr (TBU) -Li COOH
Following the method in step 2 (1), connect Fomc Phe OH to the 2-chlorotrityl chloride resin to obtain Fmoc Phe-2-CTC resin. Then, follow the method in step 2 (2) to sequentially connect Fomc Tyr (tBu) OH, Fmoc Gly OH, Fmoc Glu (otBu) Oh, fmoc gly oh, fomc li (trt) - oh nan fmoc phe -2- ctc résine, jwenn fmoc l '(trt) - gly glu (otbu) - gly glu (tbu) - pHe -2- cTc resinfMoc l' (g (gl) (gl) - gl) - gl) - gl) (gl) (gl) - gl) (gl) (gl) - gl) - gl) (gl) (gl) (gl) (gl) (gl) (gl) - Phe -2- CTC résine ak fè koupe tretman dapre metòd la nan etap 2 (3) jwenn FMOC l '(TRT) - Gly Glu (OTBU) - Gly Tr (TBU) - Phe -COOH .
Etap 7: Sentèz Exenatide
1) Rasanble epi konekte FMOC Lys (BOC) - ASN (TRT) - Gly Gly Pro SE (TBU) - SE (TBU) - Gly ala pro pro se (TBU) - MBHA résine
Retire fmoc gly pro se (tbu) se (tbu) gly ala pro pro se r (TBU) mbha résine jwenn nan etap 1 de fwa lè l sèvi avèk yon melanj de piperidine ak n, n-dimethylformamide nan yon rapò volim nan 1: {{3} N-methylpyrrolidone in a volume ratio of 0.5-1:1:2:1, as well as Fmoc Lys (Boc) Asn (Trt) Gly COOH, 1-hydroxyphenylpropanetriazole, benzotriazole-N, N, N ', N '- tetramethylurea tetrafluoroborate ak n, n ' - diisopropylethylamine te tèt anba nan tanperati chanm pou 3-4 èdtan anba pwoteksyon nitwojèn jwenn FMOC Lys (Boc) - asn (TRT) -
2) Asanble ak koneksyon exenatide
According to the assembly and connection method in step (1), sequentially assemble and connect Fmoc Val Arg (pbf) - Le Glu (otBu) - Trp Leu COOH, Fmoc Met Glu (otBu) - Glu (otBu) - Glu (otBu) - Glu (otBu) - Glu (otBu) - Ala COOH, Fmoc Thr (tBu) - Se (tBu) - Asp (otBu) - Le Se (tBu) - Lys (Boc) - Gln (Trt) - COOH, Fmoc His (Trt) - Gly Glu (otBu) - Gly Thr (tBu) - PheCOOH, Using a mixture of piperidine and N, N-dimethylformamide in a volume ratio of 1:4, Fmoc was removed twice to obtain Exenatide résine .
Sèvi ak yon solisyon koupe ki konpoze de 83% asid trifluoroacetic, 5% fenol, 4% benzil SULFIDE, 3% dlo, ak 5% triisopropylsilane pa pousantaj mas, yo te résine a nan exenatide koupe dapre Metòd la nan etap (2) ③ ③ jwennExenatide acetate.
Baj popilè: exenatide acetate cas 141732-76-5, founisè, manifaktirè, faktori, en, achte, pri, esansyèl, pou vann