Retatrutide

Retatrutide

Retatrutide

Retatrutide bụ peptide na-agbanwe agbanwe na-ezubere ndị na-anabata metabolic atọ.

 

SKU: 198881 Otu:
Kekọrịta ịhụnanya gị

Retatrutide bụ peptide agonist atọ na-anabata ihe ọhụrụ sitere na GLP-1 dual agonist Tirzepatide.. Ọ na-ahọrọ lekwasịrị anya igodo atọ ndị na-anabata metabolic: onye na-anabata glucagon (GCGR), onye na-anabata insulinotropic polypeptide na-adabere na glucose (GIPR), na glucagon-dị ka peptide-1 nnabata (GLP-1R). Ọgwụ peptide ọhụrụ a na-egosi ikike siri ike n'ịgwọ ọrịa metabolic metụtara oke ibu na ụdị 2 ọrịa shuga n'ihi nhazi ya pụrụ iche.

Ọzọkwa, Ndị ọkà mmụta sayensị mepụtara Retatrutide peptide na nke kachasị mma nke GLP-1 analog scaffold na ọ mejupụtara ya. 39 amino asịd. Usoro ya na-agụnye amino acid atọ na-abụghị nke okike iji kwalite nguzogide nbibi site na dipeptidyl peptidase-4 (DPP-4). Ọzọkwa, mmeghe nke AIB (2-Aminoisobutyric acid) na-akwalite nke ọma ma ọrụ ndu yana ọgwụ pharmacokinetics.

Na mgbakwunye, Mgbakwunye nke yinye diacid fatty C20 a lysine foduru gbatịrị ya ọkara ndụ ma mee ka profaịlụ ọgwụ ya dịkwuo mma. Ọnụ, atụmatụ ndị a dị elu na-akwado usoro ọgwụgwọ subcutaneous otu ugboro kwa izu.

Usoro

Tir-{Aịb}-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{α-M-Leo}-Leu-Asp-Lys-{diacid-C20-gamma-Glu-(EE)-Lys}-Ụzọ-Gln-{Aịb}-Ala-Phe-Ile-Glu-Tyr-Leu-Leu-Glu-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2

Nọmba CAS

2381089-83-2

Usoro ihe omimi

C221H342N46O68

Ibu molekụla

4731.33 g/mol

Nnyocha nke uru Retatrutide:

1. Na-egbochi agụụ, Na-egbu oge mkpofu afọ, ma na-akwalite insulin

1) Usoro nke ime ihe na njikwa agụụ:

Na ọmụmụ anụmanụ, ndị na-eme nchọpụta na-ebu ọnụ nwoke oke oke ibu maka 16 awa ma were agonists glucagon na-anabata ha ogologo oge, Retatrutide, Galectin peptides, yana analog GLP-1 ndị ọzọ maka njikwa ibu. A tụlere ọmụmụ ihe imefusị afọ (GE) igbu oge, ibu ahu, na nri oriri.

2)Glucose-Dabere na-egbu oge igbu oge:

Karịsịa, Retatrutide na-egbu oge GE n'ụzọ dabere na glucose. Ọ kachasị, otu na-anata 10 nmol/L Retatrutide gosipụtara mbelata kachasị elu na ịdị arọ ahụ yana mbelata kachasị na oriri nri.

3)Mmetụta Sistemụ akwara ozi etiti:

Dị ka ndị ọzọ GLP-1 agonist anabata, Retatrutide na-arụ ọrụ ozugbo Central ụjọ usoro, na-eme ka satiety dịkwuo elu ma na-ebelata nsị gastric. N'ihi ya, ọ na-akwado ọgwụgwọ oke ibu dị irè.

4) Nsonaazụ mbelata ịdị arọ nke nnwale ụlọ ọgwụ:

Ọmụmaatụ, a Phase 2 Nnwale ụlọọgwụ kọrọ na mbelata oke ibu na oke ibu na ndị okenye buru ibu: 17.5% na 24 izu na 24.4% na 48 izu.

2. Ụdị ọgwụgwọ 2 Ọrịa shuga mellitus

  • Usoro ọmụmụ nke usoro 1b nke ukwuu metụtara ụdị 2 Ndị na-arịa ọrịa shuga na-anata dose nke Retatrutide kwa izu ma ọ bụ ọgwụ ndị ọzọ na-ebelata glucose, na otu njikwa na-anata enweghị ọgwụgwọ.
  • N'ụzọ dị ịrịba ama, Emezuola Retatrutide 100% nke ebumnuche ọnwụ arọ, tụnyere naanị 2.1% n'ime otu njikwa. Na ntule ndịiche, Ọ dịghị ọgwụ ọrịa shuga ọzọ enwetara 50% arụmọrụ.
  • Nchọpụta ndị a gosipụtara n'ụzọ doro anya arụmọrụ kacha mma Retatrutide na njikwa ụdị 2 ọrịa shuga mellitus. Agbanyeghị, mmetụta kachasị emetụta bụ eriri afọ.
  • N'otu oge ahụ, na oke ibu, Ọgwụgwọ retatrutide mekwara ka mbelata oke ibu 48 izu.

3. Na-akwalite mmefu ike

  • Dị ka agonist atọ, Retatrutide na-eme ka onye na-anabata glucagon rụọ ọrụ dịka glucagon. Kpọmkwem, ọ na-akpalite thermogenesis ozugbo na mmebi abụba.
  • Ọ dị mkpa ịmara na ndị na-anabata glucagon dị na imeju na anụ ahụ adipose. Site na ịgbalite ndị nnabata ndị a, Retatrutide na-abawanye mmefu ike na mmepụta okpomọkụ na imeju.
  • N'ihi ya, ọ na-akwalite ọnụego metabolic ma na-akwalite abụba oxidation.

4. Na-ebelata mbufụt ma na-agwọ ọrịa imeju abụba abụba

1)Uru mgbochi mkpali:

Retatrutide na-enye uru mgbochi mkpali akụkụ dị iche iche. Dị ka ọmụmaatụ, ọmụmụ na-egosi na ọ na-eme ka nnabata glucose dịkwuo mma, na-ebelata ibu ahụ na oke abụba, ma na-akwalite profaịlụ lipid.

2) Mweghachi nke Steatohepatitis na ụmụ oke:

Na mgbakwunye, ọ na-atụgharị steatohepatitis na oke nwanyi, na-akwado mkpebi nke ọrịa imeju abụba abụba site na ibelata steatosis imeju. N'otu ọmụmụ ihe, ụmụ oke ndị na-eme nchọpụta nyere oke abụba nri, nri shuga dị elu maka 38 Izu izu natara subcutaneous Retatrutide, na ndị nchọpụta buo ọnụ ha 4 awa.

E mesịa, histological analysis gosiri n'elu 80% nwere ezi steatohepatitis. Dị mkpa, Retatrutide kwalitere ọnọdụ ahụ dabere na dose, na ụfọdụ ụmụ nwanyị na-egosi ngbanwe zuru oke.

3) Nsonaazụ nyocha akụkọ ihe mere eme:

N'ọnwụnwa mmadụ ọzọ, ndị nchọpụta mesoo 98 ndị sonyere nwere ≥10% abụba imeju. Mgbe 48 izu nke ọgwụgwọ Retatrutide, abụba imeju belatara site na 51.3% (1 mg), 59% (4 mg), na 86% (12 mg), atụlere yana 4.6% n'ime otu njikwa.

N'ikpeazụ, niile emeso ndị ọrịa nweta nkịtị imeju abụba etoju.

COA

HPLC

MS

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