Product Description
Retatrutide inyowani katatu agonist peptide yakanangana neglucagon receptor (GCGR), glucose-inotsamira insulinotropic polypeptide receptor (GIPR), uye glucagon-like peptide-1 receptor (GLP-1R). Retatrutide inomutsa GCGR yemunhu, GIPR, uye GLP-1R ine EC50 tsika dze5.79, 0.0643, uye 0.775 nM, zvichiteerana, uye mbeva GCGR, GIPR, uye GLP-1R ine EC50 tsika dze 2.32, 0.0.0. Inoshanda sechinhu chakakosha chekutsvagisa mukudzidza kwekufutisa uye metabolic kusagadzikana.
Retatrutide inonyatso mutsa iyo GLP-1R yekusaina nzira uye inomutsa glucose-inotsamira insulin secretion nekuita pane ese GIP uye GLP-1 receptors. Iyi peptide yekugadzira inoratidza yakasimba hypoglycemic zvimiro uye yakagadziridzwa senge anti-diabetic komboni yeType 2 Diabetes (T2D). Inosimudzira kuburitswa kwe insulin uye inodzvanya glucagon secretion nenzira inoenderana neglucose.
Uyezve, Retatrutide yakaratidzwa kunonoka kubuda kwegastric, kuderedza kutsanya uye postprandial glucose mazinga, kuderedza kudya kwekudya, uye kukonzera kurasikirwa kwehuremu hwemuviri kune vanhu vane T2D.
Biological Activity
Retatrutide (LY3437943) ndeye imwechete lipid-conjugated peptide inoshanda seyakasimba agonist yeGCGR yemunhu, GIPR, uye GLP-1R. Kuenzaniswa neyakazvarwa glucagon yemunhu uye GLP-1, Retatrutide inoratidza yakaderera potency paGCGR uye GLP-1R (0.3 × uye 0.4 × 0.4 ×, zvichiteerana) asi inoratidza yakawedzera kuwedzera potency (8.9 ×) paGIPR kana ichienzaniswa neglucose-inotsamira insulinotropic polypeptide (GIP).
Nzira Yekuita
Muzvidzidzo zvinosanganisira mbeva dzeshuga dzine nephropathy, Retatrutide manejimendi yakaderedza zvakanyanya albuminuria uye yakavandudza glomerular filtration rate. Izvi zvinodzivirira zvinokonzerwa nekushandiswa kweiyo GLP-1R / GR-inotsamira nzira yechiratidzo, iyo inopindirana nekurwisa-kuzvimba uye anti-apoptotic zviito mune renal tishu.
Retatrutide zvakare inogadzirisa zvakananga glomerular permeability, inosimudzira weti yekuisa pfungwa. Zvakawanikwa zvekutanga zvinoratidza kuti, kana zvichienzaniswa neakajairika chirwere cheitsvo kurapa senge ACE inhibitors uye ARBs, Retatrutide inoburitsa yakawedzera kuderedzwa kwealbuminuria mushure memavhiki mana chete ekurapa. Uyezve, yakaratidza kushanda kukuru mukuderedza systolic blood pressure kupfuura ACE inhibitors kana ARBs, pasina migumisiro yakaipa yakaonekwa.
Side Effects
Izvo zvinowanzoitika mhedzisiro yeRetatrutide ndeye gastrointestinal mune zvakasikwa, kusanganisira kusvotwa, manyoka, kurutsa, uye kuvimbiswa. Zviratidzo izvi kazhinji zvakapfava kusvika pakati nepakati uye zvinowanzogadzirisa nekuderedzwa kwedosi. Inenge 7% yezvidzidzo zvakare yakashuma kunzwa kweganda kurira. Kuwedzera kwehuwandu hwemoyo kwakaonekwa pamasvondo e24 mumapoka epamusoro-dose, ayo akazodzokera kumazinga ekutanga.