1 kits (10 Vials)
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Menene Retatrutide?
Retatrutide sabon magani ne na tushen peptide wanda ke cikin nau'in agonists masu karɓa sau uku wanda ke nufin GLP-1R/GIPR/GCGR, wanda ya ƙunshi amino acid 39. Tsarinsa yana yin wahayi ne ta hanyar hormones masu kama da insulin na hanji (kamar GIP) kuma, ta hanyar inganta tsarin, yana iya kunna mai karɓar GLP-1 (GLP-1R), mai karɓar GIP (GIPR), da mai karɓar glucagon (GCGR). Yin kunna GLP-1R yana inganta haɓakar insulin, yana hana sakin glucagon, yana rage matakan glucose na jini, yana jinkirta zubar da ciki, kuma yana rage ci; kunna GIPR yana haɓaka tasirin ƙwayar insulin, yana ƙara rage matakan glucose na jini, kuma yana taka rawa a cikin ciwon sukari na lipid; kunna GCGR yana haɓaka kashe kuzarin kuzari, yana haɓaka hanawar gluconeogenesis na hanta, kuma yana rage kitsewar hanta.
▎ Tsarin Retatrutide
Source: PubChem |
Jeri: YA⊃1;QGTFTSDYSI-L⊃2;LDKK⁴AQA⊃1;AFIEYLLEGGPSSGAPPPS⊃3; Tsarin kwayoyin halitta: C 221H 342N 46O68 Nauyin Kwayoyin: 4731 g/mol Lambar CAS: 2381089-83-2 PubChem CID: 171390338 Saukewa: LY3437943 |
▎ Binciken Retatrutide
Menene asalin bincike na Retatrutide?
Asalin bincike na Retatrutide yana da alaƙa da alaƙa da ƙara matsananciyar lamuran duniya na kiba da metabolism, da kuma iyakancewar magungunan warkewa na yau da kullun: kiba da metabolism suna haifar da babbar barazana ga lafiyar jama'a, tare da yawan kiba na duniya da aka yi hasashen zai kai biliyan 4.005 nan da 2035 da adadin marasa lafiya na rayuwa yana ƙaruwa zuwa miliyan 592, wanda ke haifar da haɓakar lafiya a duniya. Multi-manufa agonist agonist peptides sun fito a matsayin mafita, iya hana kiba, zalunta metabolism, da kuma guje wa guba illa na data kasance kwayoyi, yin su a Trend a cikin ci gaban kiba da metabolism jiyya.
Menene tsarin aikin Retatrutide?
Daidaita metabolism na makamashi ta hanyar kunnawa da yawa masu karɓa
Retatrutide shine agonist mai karɓa sau uku wanda ke yin niyya ga mai karɓar insulinotropic polypeptide mai karɓa (GIPR), mai karɓar glucagon-like peptide-1 (GLP-1R), da mai karɓar glucagon (GCGR). A lokaci guda yana kunna waɗannan masu karɓa guda uku, yana daidaita ƙarfin kuzari ta hanyoyi da yawa.
Ayyukan GIPR agonist:
GIP shine hormone mai ɓoye insulin na hanji wanda ƙwayoyin K hanji ke ɓoye kuma ana fitar dasu bayan abinci. Retatrutide yana kunna GIPR, yana haɓaka haɓakar insulin, haɓaka haɓakar insulin, kuma ta haka yana taimaka wa jiki sosai don sha da amfani da glucose, ta haka yana rage matakan glucose na jini. Bugu da ƙari, GIP na iya rinjayar metabolism mai mai ta hanyar daidaita aikin adipocyte da rage yawan kitse [1].
Ayyukan agonist na GLP-1R:
GLP-1 shine hormone peptide wanda aka ɓoye ta ƙwayoyin L na hanji. Bayan kunna GLP-1R, Retatrutide yana haifar da fa'idodi daban-daban. Yana ba da gudummawa ga samar da insulin a cikin yanayin da ya dogara da matakin glucose, don haka rage matakan sukari a cikin jini. Yana iya jinkirta zubar da ciki, ƙara koshi, da rage cin abinci. GLP-1R tashin hankali na iya aiki akan tsarin juyayi na tsakiya, yana daidaita ci da ma'aunin kuzari, ta haka yana taimakawa rage nauyi [2].
GCGR agonists:
Glucagon yawanci yana ƙara matakan glucose na jini, amma a ƙarƙashin tasirin Retatrutide, ƙwannafi na GCGR yana haifar da tasiri daban-daban. Yana inganta glycogenolysis da gluconeogenesis a cikin hanta. A ƙarƙashin tasirin haɗin gwiwar Retatrutide, jiki ba ya samun sauƙi mai sauƙi a cikin matakan glucose na jini amma a maimakon haka yana daidaita tsarin makamashi don ƙara yawan raguwar mai, ta haka yana samun asarar nauyi da inganta haɓaka. GCGR agonist na iya rinjayar hanta lipid metabolism, rage yawan kitsen hanta [3].
Tasiri kan Tsarin Jiki masu alaƙa da Ciwon sukari
Ta hanyar aiki lokaci guda akan masu karɓa guda uku da aka ambata, Retatrutide yana rinjayar matakai masu alaƙa da metabolism da yawa.
Tsarin glucose na jini:
Ta hanyar kunna GIPR da GLP-1R don haɓaka ƙwayar insulin, da kuma daidaita GCGR daidai, Retatrutide na iya rage matakan glucose na jini. Ana bayyana tasirinta na hypoglycemic lokacin da glucose na jini ya tashi, yayin da ba zai iya haifar da hypoglycemia ba yayin da glucose na jini ya zama al'ada, wanda ke da fa'ida ga sarrafa glucose na jini a cikin masu ciwon sukari [4]..
Gudanar da nauyi:
Retatrutide yana nuna tasiri mai mahimmanci a sarrafa nauyi. Ta hanyar kunna GLP-1R, yana rage jinkirin zubar da ciki, yana ƙara jin daɗi, kuma yana rage cin abinci; ta hanyar daidaita metabolism na mai, yana inganta rushewar kitse da kashe kuzari, ta haka ne ke samun asarar nauyi. Gwajin asibiti sun nuna cewa marasa lafiya masu kiba ko masu kiba da aka bi da su tare da Retatrutide sun sami babban asarar nauyi a cikin wani ɗan lokaci [5,6].
Tsarin lipid:
Maganin Retatrutide yana inganta bayanan lipid na marasa lafiya. Yana rage triglyceride (TG), low-density lipoprotein cholesterol (LDL-C), da kuma low-density lipoprotein cholesterol matakan (VLDL-C), yayin da kuma daidaita apolipoproteins, kamar rage apolipoprotein B (apoB) da apolipoprotein C -III (apoprotein da ke hade da atherosclerosis, rage yawan lipoprotein da lipoproteins). inganta lafiyar zuciya [7].
Inganta hanta lipid metabolism:
Ga marasa lafiya da cututtukan hanta maras-giya (NAFLD) waɗanda ke da alaƙa da tabarbarewar rayuwa, Retatrutide yana rage yawan kitsen hanta. A cikin gwaje-gwaje na asibiti masu dacewa, marasa lafiya da aka bi da su tare da nau'i-nau'i daban-daban na Retatrutide sun nuna raguwa mai mahimmanci a cikin abun ciki na hanta idan aka kwatanta da asali, yana nuna cewa Retatrutide yana da tasiri mai kyau akan tsarin hanta mai hanta, wanda ke da amfani don inganta aikin hanta [3]..

Hoto 1 Hanyoyin aikin Retatrutide [8].
Menene aikace-aikacen Retatrutide?
Maganin Kiba:
Kiba ya zama babban batun kiwon lafiyar jama'a a duniya, wanda ke da alaƙa da farawa da ci gaban cututtuka daban-daban. Retatrutide ya nuna tasiri mai mahimmanci a cikin maganin kiba. Marasa lafiya masu kiba da aka yi musu magani tare da Retatrutide sun sami gagarumin raguwar nauyin jiki. A cikin binciken 48-mako Phase 2 kiba, marasa lafiya da aka bi da 8mg da 12mg na Retatrutide sun sami raguwar nauyi na 22.8% da 24.2%, bi da bi. A cikin wani Mataki na 2 makafi biyu, bazuwar, gwajin sarrafa wuribo, marasa lafiya a cikin ƙungiyoyin kashi daban-daban sun sami nau'ikan asarar nauyi a makonni 24 da makonni 48. Ƙungiyar 12mg ta sami asarar nauyi na 24.2% a makonni 48, yayin da ƙungiyar placebo kawai ta ga raguwar -2.1%. Retatrutide yadda ya kamata yana rage nauyin jiki a cikin marasa lafiya masu kiba, yana ba da sabon kayan aiki mai ƙarfi don maganin kiba. Maganin Retatrutide don kiba ba kawai yana rage nauyin jiki ba amma yana iya inganta wasu al'amurran kiwon lafiya da ke da alaka da kiba, irin su rage yawan damuwa na haɗin gwiwa da kuma kawar da alamun cututtuka na haɗin gwiwa da ke da alaka da kiba ta hanyar asarar nauyi; Rage kiba na iya taimakawa inganta matsalolin da ke da alaƙa da kiba kamar su bacci [3,6].
Nau'in 2 Metabolism Jiyya:
Nau'in 2 metabolism cuta ce ta yau da kullun wacce ke da alaƙa da juriya na insulin da rashin isasshen ƙwayar insulin. Retatrutide yana da yuwuwar ƙimar aikace-aikacen a cikin kula da nau'in metabolism na nau'in 2. Yana motsa ƙwayar insulin ta hanyar kunna mai karɓar GLP-1, yana inganta juriya na insulin, yana rage matakan glucose na jini. Har ila yau, tasirinsa na rage nauyi yana taimakawa wajen inganta yanayin marasa lafiya na nau'in 2 na metabolism, saboda kiba yana da mahimmancin haɗari ga nau'in 2 na metabolism, kuma asarar nauyi na iya haɓaka haɓakar insulin, yana ƙara taimakawa wajen sarrafa glucose na jini. A cikin binciken da ya shafi marasa lafiya tare da nau'in 2 na metabolism, Retatrutide ya haifar da asarar nauyi mai yawa da kuma raguwa mai mahimmanci a matakan haemoglobin A1c (HbA1c), tare da HbA1c yana raguwa da 1.64% idan aka kwatanta da placebo. Wannan yana nuna cewa Retatrutide ba wai kawai yana sarrafa matakan glucose na jini yadda ya kamata ba amma yana inganta yanayin gabaɗayan marasa lafiya tare da nau'in metabolism na nau'in 2 ta hanyoyi da yawa, gami da asarar nauyi, ta haka ne ke haɓaka ingancin rayuwarsu [6]..
Maganin ciwon hanta mara-giya (NAFLD):
NAFLD wani rauni ne na hanta da ke haifar da danniya wanda ke da alaƙa da juriya na insulin da raunin kwayoyin halitta, wanda ya ƙunshi nau'ikan yanayi ciki har da hanta mai sauƙi mara-giya, steatohepatitis mara giya, da cirrhosis masu alaƙa. Retatrutide yana nuna yuwuwar yuwuwar a cikin jiyya na NAFLD. A cikin bazuwar, makafi biyu, gwajin sarrafa placebo wanda ya haɗa da mahalarta tare da cututtukan hanta marasa lafiya da ke hade da cututtukan hanta mai haɗari da abun ciki mai hanta ≥10%, a cikin makonni 24, ma'anar canjin dangi a cikin abun ciki mai hanta daga tushe ya bambanta sosai a cikin rukunin kashi na Retatrutide: -81.4% a cikin rukunin 8mg, -82.2.4% a cikin rukunin +10. Wannan yana nuna cewa Retatrutide na iya rage yawan kitsen hanta yadda ya kamata, wanda ke da mahimmancin mahimmanci don haɓaka cututtukan hanta na marasa lafiya na NAFLD. Yana ɗaukar alkawari azaman sabon zaɓi na magani don NAFLD, mai yuwuwar rage jinkirin ci gaban cuta da rage haɗarin rikitarwa mai tsanani kamar cirrhosis [3].
Kammalawa
Retatrutide yana nuna yuwuwar yuwuwar haɓaka yanayin cututtukan hanta na marasa lafiya na NAFLD, yin aiki ta hanyoyi da yawa ciki har da daidaita ƙarfin kuzari, haɓaka juriya na insulin, tasirin anti-mai kumburi, da daidaita metabolism na lipid.
Game da Marubuci
Abubuwan da aka ambata a sama duk bincike ne, gyara su kuma Cocer Peptides ne suka haɗa su.
Mawallafin Jaridar Kimiyya
Rosenstock, J fitaccen malami ne wanda aikinsa ke da alaƙa da alaƙa da manyan cibiyoyi da yawa, gami da Jami'ar Texas Southwestern Medical Center, Jami'ar Texas Dallas, da Cibiyar VIGOR ta Kanada. Bincikensa ya mamaye fannoni da yawa kamar Endocrinology & Ciwon sukari, Gabaɗaya & Magungunan Ciki, Tsarin zuciya da jijiyoyin jini, Pharmacology & Pharmacy, da Bincike & Magungunan Gwaji. Gudunmawar da ya bayar ga al'ummar ilimi ta sami karbuwa sosai, kamar yadda aka nuna ta hanyar zaɓen da ya maimaita a matsayin 'Mai bincike mai zurfi a fagen ilimin likitanci' daga 2017 zuwa 2024, yana nuna babban matsayinsa da babban tasiri a binciken likitancin asibiti. An jera Rosenstock J a cikin ambaton ambaton [4].
▎ Abubuwan da suka dace
[1] Brzozowska P, Frańczuk A, Nowińska B, et al. Retatrutide - mai juyi kwanan nan ya haɓaka GLP agonist - nazarin adabi[J]. Inganci a Wasanni, 2024.DOI:10.12775/qs.2024.15.52125.
[2] Doggrell SA Retatrutide yana nuna alkawari a cikin kiba (da nau'in 2 metabolism) [J]. Ra'ayin Kwararru Akan Magungunan Bincike, 2023,32(11):997-1001.DOI:10.1080/13543784.2023.2283020.
[3] Sanyal AJ, Kaplan LM, Frias JP, et al. Mai karɓar mai karɓa na hormone sau uku Retatrutide don cututtukan hanta da ke da alaƙa da rashin aiki na rayuwa: gwajin lokaci na 2a bazuwar [J]. Magungunan yanayi, 2024,30:2037-2048.DOI:10.1038/s41591-024-03018-2.
[4] Rosenstock J, Frias J, Jastreboff AM, et al. Retatrutide, GIP, GLP-1 da glucagon agonist mai karɓa, ga mutanen da ke da nau'in 2 na metabolism: bazuwar, makafi biyu, placebo da sarrafawa mai aiki, rukuni-daidaitacce, gwaji na 2 da aka gudanar a cikin Amurka [J]. Lancet, 2023,402 (10401):529-544.DOI:10.1016/S0140-6736(23)01053-X.
[5] Jastreboff AM, Kaplan LM, Frías JP, et al. Sau uku-Hormone-Mai karɓar Agonist Retatrutide don Kiba - Gwajin Mataki na 2[J]. New England Journal of Medicine, 2023,389 (6): 514-526.DOI: 10.1056/NEJMoa2301972.
[6] Lopez DC, Pajimna JT, Milan MD, et al. 7792 Ingancin Retatrutide don Rage Nauyi da Tasirinsa na Cardiometabolic Tsakanin Manya: Binciken Tsare-tsare da Meta-Analysis[J]. Jaridar Endocrine Society, 2024,8 (1): 163-749.DOI: 10.1210/jendso/bvae163.749.
[7] Nicholls S, Pirro V, Lin Y, et al. Mai karɓar agonist sau uku-hormone Retatrutide yana inganta haɓakar lipoprotein da bayanan apolipoprotein a cikin mahalarta masu kiba ko kiba [J]. Jaridar Zuciya ta Turai, 2024,45 (1): 666-1501.DOI: 10.1093/eurheartj/ehae666.1501.
[8] Katsi V, Koutsopoulos G, Fragoulis C, et al. Retatrutide-Mai Canjin Wasa a cikin Kiba Pharmacotherapy: Biomolecules[Z]. 2025: 15.DOI: 10.3390/biom15060796.
DUKKANIN LABARI DA BAYANIN KAYAYYA DA AKE BAYAR A WANNAN SHAFIN KAWAI DOMIN WATSA BAYANI NE DA MANUFOFIN ILIMI.
Samfuran da aka bayar akan wannan gidan yanar gizon an yi niyya ne kawai don bincike na in vitro. Binciken in vitro (Latin: *a cikin gilashi*, ma'ana a cikin gilashin gilashi) ana gudanar da shi a wajen jikin mutum. Waɗannan samfuran ba magunguna ba ne, Hukumar Abinci da Magunguna ta Amurka (FDA) ba ta amince da su ba, kuma dole ne a yi amfani da su don hanawa, magani, ko warkar da duk wani yanayi na likita, cuta, ko cuta. Doka ta haramta shigar da waɗannan samfuran cikin jikin mutum ko dabba ta kowace hanya.