Retatrutide

Retatrutide

Retatrutide

Retatrutide ke peptide ea phetoho e shebileng li-receptor tse tharo tsa bohlokoa tsa metabolic.

 

SKU: 198881 Sehlopha:
Arolelana lerato la hau

Retatrutide ke peptide e ncha ea li-agonists tse tharo tse tsoang ho GLP-1-based dual agonist Tirzepatide.. E khetha ka ho khetheha linotlolo tse tharo li-receptor tsa metabolism: mokelikeli oa glucagon (GCGR), insulinotropic polypeptide receptor e itšetlehileng ka tsoekere (GIPR), le glucagon-joaloka peptide-1 receptor (GLP-1R). Setlhare sena se secha sa peptide se bonts'a bokhoni bo matla ba ho alafa mathata le mofuta o amanang le botenya 2 lefu la tsoekere ka lebaka la sebopeho sa eona se ikhethang.

Ho feta moo, Bo-rasaense ba thehile peptide ea Retatrutide holim'a scaffold e ntlafalitsoeng ea analog ea GLP-1 mme e na le 39 li-amino acid. Tatelano ea eona e kenyelletsa li-amino acid tse tharo tseo e seng tsa tlhaho ho matlafatsa ho hanyetsa ho senyeha ka dipeptidyl peptidase-4 (DPP-4). Ho feta moo, kenyelletso ea AIB (2-Aminoisobutyric acid) e ntlafatsa haholo ts'ebetso ea bioloji le pharmacokinetics.

Ho phaella moo, sehokelo sa ketane ea C20 e mafura a diacid a lysine masalla a atolosa lona halofo ea bophelo le ho ntlafatsa boemo ba eona ba meriana. Mmoho, likarolo tsena tse tsoetseng pele li tšehetsa dosing ea subcutaneous hang ka beke.

Tatelano

Tyr-{Aib}-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{α-Me-Leo}-Leu-Asp-Lys-{diacid-C20-gamma-Glu-(EE)-Lys}-Path-Gln-{Aib}-Ala-Phe-Ile-Glu-Tyr-Leu-Leu-Glu-Gly-Gly-Pro-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2

Nomoro ea CAS

2381089-83-2

Foromo ea limolek'hule

C221H342N46O68

Boima ba Molek'hule

4731.33 g/mol

Lipatlisiso tsa Melemo ea Retatrutide:

1. E Hatella Takatso, E Lieha ho Hlakola Maleng, le ho susumetsa Insulin

1)Mokhoa oa Ts'ebetso ho Taolo ea Takatso ea Lijo:

Thutong ea liphoofolo, bafuputsi ba itima lijo banna litoeba tse nonneng bakeng sa 16 lihora tse ngata le ho li phekola ka li-agonists tsa nako e telele tsa glucagon, Retatrutide, li-peptide tsa galectin, le li-analogue tse ling tsa GLP-1 bakeng sa taolo ea boima ba 'mele. Thuto e hlahlobile ho ntsha mala (GE) tieho, boima ba mmele, le ho ja lijo.

2)Tieho ea ho Ntša Ka Gastric e Itšetlehileng ka Glucose:

Ka ho khetheha, Retatrutide e liehile GE ka mokhoa o itšetlehileng ka tsoekere. Ka ho khetheha, sehlopha se amohelang 10 nmol/L Retatrutide e bontšitse phokotso e phahameng ka ho fetisisa ea boima ba 'mele le ho fokotseha ho hoholo ha tšebeliso ea lijo.

3)Liphello tsa Tsamaiso ea Methapo e Bohareng:

Hoa tšoana le ho tse ling GLP-1 receptor agonist, Retatrutide e sebetsa ka kotloloho ho tsamaiso ea methapo e bohareng, ho matlafatsa ho kgora le ho fokotsa ho ntsha mala. Ka hoo, e tšehetsa phekolo e atlehang ea botenya.

4)Liphetho tsa Tahlehelo ea Boima ba Teko ea Kliniki:

Ka mohlala, a Mokhahlelo 2 teko ea tleliniki e tlalehile tahlehelo e kholo ea boima ba 'mele ho batho ba baholo ba batenya le ba batenya: 17.5% ho 24 libeke le 24.4% ho 48 libeke.

2. Mefuta ea litloaelo 2 Lefu la tsoekere

  • Boithuto ba litekanyetso tse ngata tse nyolohang tsa Mokhahlelo oa 1b bo kenyelelitse mofuta 2 Bakuli ba nang le lefu la tsoekere ba fuoa litekanyetso tsa beke le beke tsa Retatrutide kapa lithethefatsi tse ling tse theolang tsoekere, ka sehlopha sa taolo se sa fumaneng kalafo.
  • Ka mokhoa o tsotehang, Retatrutide e fihletsoe 100% ea sepheo sa ho theola boima ba 'mele, bapisoa le feela 2.1% sehlopheng sa taolo. Ka papiso, ha ho setlhare se seng sa lefu la tsoekere se fihletsoeng 50% katleho.
  • Liphuputso tsena li bontša ka ho hlaka katleho e phahameng ea Retatrutide ho laola mofuta 2 lefu la tsoekere. Leha ho le joalo, litla-morao tse atileng haholo e ne e le mala.
  • Ka nako e tšoanang, ho batho ba baholo ba batenya, Phekolo ea Retatrutide e boetse e lebisitse ho theoheng ha boima ba 'mele ho feta 48 libeke.

3. E Khothalletsa Litšenyehelo tsa Matla

  • Joalo ka agonist e meraro, Retatrutide e kenya tšebetsong glucagon receptor ka mokhoa o ts'oanang le glucagon. Ka ho toba, ka ho toba e susumetsa thermogenesis le ho senyeha ha mafura.
  • Ke habohlokoa ho hlokomela hore li-receptor tsa glucagon li teng sebeteng le lisele tsa adipose. Ka ho kenya tšebetsong li-receptor tsena, Retatrutide e eketseha litšenyehelo tsa matla le tlhahiso ea mocheso sebeteng.
  • Ka lebaka leo, e matlafatsa metabolism le ho khothalletsa oxidation ea mafura.

4. E Fokotsa ho Ruruha Le ho Phekola Mafura a Lefu la Sebete

1)Melemo e Khahlanong le Ho ruruha:

Retatrutide e fana ka melemo e mengata e khahlanong le ho ruruha. Mohlala, Liphuputso li bonts'a hore e ntlafatsa mamello ea glucose, e fokotsa boima ba 'mele le boima ba mafura, mme e ntlafatsa boemo ba lipids.

2) Phetoho ea Steatohepatitis ho litoeba:

Ho phaella moo, e a furalla steatohepatitis ho litoeba tse tšehali, ho tšehetsa qeto ea lefu la sebete sa mafura ka ho fokotsa sebete sa steatosis. Thutong e 'ngoe, litoeba tseo bafuputsi ba li fepang mafura a mangata, lijo tse nang le tsoekere e ngata bakeng sa 38 Libeke li ile tsa amohela Retatrutide ea subcutaneous, 'me bafuputsi ba li itima lijo bakeng sa 4 lihora.

Kamora moo, tlhahlobo ea histological e bontšitse 80% o na le steatohepatitis e hlakileng. Habohlokoa, Retatrutide e ntlafalitse boemo ho latela tekanyetso, ka tse ding tse tshehadi tse bontshang phetoho e felletseng.

3)Liphetho tsa Tlhahlobo ea Histori:

Tekong e nngwe ya motho, bafuputsi ba phekoloa 98 barupeluoa ba nang le ≥10% mafura a sebete. Kamora 48 libeke tsa phekolo ea Retatrutide, mafura a sebete a fokotsehile ka 51.3% (1 mg), 59% (4 mg), le 86% (12 mg), ha ho bapisoa le 4.6% sehlopheng sa taolo.

Qetellong, bakuli bohle ba tšoaroang ba fihletse maemo a tloaelehileng a mafura a sebete.

COA

HPLC

MOF

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