Retatrutide (Synonyms: LY3437943) raw material

DescriptionRetatrutide (LY3437943) is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide binds human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide can be used for the research of obesity.For research use only. We do not sell to patients.DescriptionRetatrutide (LY3437943) is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide binds human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide can be used for the research of obesity[1].IC50 & TargetEC50 (for human): 5.79 (GCGR), 0.0643 (GIPR), 0.775 nM (GLP-1R) [1]. EC50 (for mouse): 2.32 (GCGR), 0.191 (GIPR), 0.794 nM (GLP-1R) [1]. Ki (for human): 5.6 (GCGR), 0.057 (GIPR), 7.2 nM (GLP-1R) [1]. Ki (for mouse): 73 (GCGR), 2.8 (GIPR), 1.3 nM (GLP-1R)[1].In VitroRetatrutide (LY3437943) has efficacy for human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively[1]. Retatrutide has efficacy for mouse GCGR, GIPR, and GLP-1R with EC50 values of 2.32, 0.191 and 0.794 nM, respectively[1]. Retatrutide has binding affinity for human GCGR, GIPR, and GLP-1R with Ki values of 5.6, 0.057 and 7.2 nM, respectively[1]. Retatrutide has binding affinity for mouse GCGR, GIPR, and GLP-1R with Ki values of 73, 2.8 and 1.3 nM, respectively[1].MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.Retatrutide Related AntibodiesGLP-1R AntibodyGlucagon Antibodygamma Sarcoglycan Antibody (YA1357)delta Sarcoglycan Antibody (YA3326)In VivoRetatrutide (LY3437943) (s.c.; 47 g/kg; single) engages GCGR in vivo and can improve glucose tolerance in an ipGTT through either the GIP or GLP-1 receptors[1]. Retatrutide (s.c.; 10 mL/kg; cycle every 3 days; for 21 days) causes great body weight loss and increases energy expenditure through glucagon receptor activatio[1]. Retatrutide has safety and tolerability[1].MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.Animal Model:Male CD-1 mice[1]Dosage:47 g/kgAdministration:Subcutaneous administration, singleResult:AUClast, ng*h/mLAUC0-?, ng*h/mLCmax, ng/mLTmax, ht1/2, hCLF, mL/h/kg41135419051680122111.22Clinical TrialNCT NumberSponsorConditionStart DatePhaseNCT05931367Eli Lilly and CompanyObesity|Overweight|Osteo Arthritis KneeAugust 28, 2023Phase 3NCT05929066Eli Lilly and CompanyObesity|Overweight|Knee Pain Chronic|Knee Osteoarthritis|Obstructive Sleep ApneaAugust 7, 2023Phase 3NCT05882045Eli Lilly and CompanyObesity|Cardiovascular DiseasesMay 30, 2023Phase 3NCT05611957Eli Lilly and CompanyHealthy|Renal InsufficiencyNovember 16, 2022Phase 1NCT04881760Eli Lilly and CompanyObesity|OverweightMay 20, 2021Phase 2NCT05445232Eli Lilly and CompanyObesityJuly 8, 2022Phase 1NCT04823208Eli Lilly and CompanyDiabetes Mellitus, Type 2May 24, 2021Phase 1NCT05936151Eli Lilly and CompanyOverweight or Obesity|CKD|Type 2 DiabetesJuly 20, 2023Phase 2NCT06003465Eli Lilly and CompanyHealthyAugust 29, 2023Phase 1NCT05916560Eli Lilly and CompanyHealthy|Hepatic InsufficiencyJuly 13, 2023Phase 1NCT05929079Eli Lilly and CompanyType 2 Diabetes|Obesity|Overweight|Obstructive Sleep ApneaJuly 11, 2023Phase 3NCT05548231Eli Lilly and CompanyOverweight|ObesityOctober 24, 2022Phase 1NCT04143802Eli Lilly and CompanyDiabetes Mellitus, Type 2December 18, 2019Phase 1NCT05959096Eli Lilly and CompanyHealthyJuly 18, 2023Phase 1NCT03841630Eli Lilly and CompanyHealthyMarch 13, 2019Phase 1NCT04867785Eli Lilly and CompanyType 2 DiabetesMay 13, 2021Phase 2Molecular Weight4731.33FormulaC221H342N46O68CAS No.2381089-83-2AppearanceSolidColorWhite to off-whiteSequenceTyr-{Aib}-Gln-Gly-Thr-Phe-Thr-Ser-Asp-Tyr-Ser-Ile-{?-Me-Leu}-Leu-Asp-Lys-{diacid-C20-gamma-Glu-(AEEA)-Lys}-Ala-Gln-{Aib}-Ala-Phe-Ile-Glu-Tyr-Leu-Leu-Glu-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2ShippingRoom temperature in continental US; may vary elsewhere.StorageSealed storage, away from moisture and light, under nitrogenPowder-80°C2 years-20°C1 year*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)