English synonyms :Eloralintide
English synonyms:Eloralintide;AMY1176;Eloralintide,LY3841136;LY3841136
CAS number :2883634-40-8
Molecular formula : C201H319N49O65S2
Molecular weight :4526.10
Properties: White to off-white
Content: ≥98%(HPLC) Professional scientific accurate detection
Function: Used in foreign trade export, scientific research and chemical reagents and other fields
Packing: 1G 100G 500G 1KG
Storage: Dry sealed with dark light -20℃ storage period of 2 years
Structural formula:
Eloralintide use and synthesis method
Intro
Eloralintide is an amylin analog and a selective, long-acting amylin receptor agonist. It acts by selectively activating the human amylin 1 receptor (AMY1R), with a potency for AMY1R activation that is 12-fold greater than that for the calcitonin receptor, aiming to reduce calcitonin-related side effects. The compound has been structurally modified to extend its half-life, supporting once-weekly subcutaneous administration, while also reducing immunogenicity and the risk of self-aggregation into amyloid fibrils. In Phase II clinical trials, once-weekly administration for 48 weeks resulted in an average weight loss of approximately 20% in the highest-dose group, with the most common treatment-emergent adverse events being nausea and fatigue, most of which were mild to moderate.
Peculiarity
Eloralintide is an amylin receptor agonist, a long-acting synthetic amylin analog that has been structurally modified to exert its pharmacological activity by selectively activating the amylin 1 receptor (AMY1R). Its potency for activating human AMY1R is 12-fold greater than that for the calcitonin receptor, and this high selectivity is intended to reduce potential side effects associated with calcitonin activity. Eloralintide extends its half-life through reversible binding to albumin via a C20 fatty diacid side chain, supporting once-weekly subcutaneous administration. In addition, the compound has been structurally optimized to reduce the risk of immunogenicity as well as the risk of self-aggregation into amyloid fibrils. In preclinical studies, eloralintide induced significantly less conditioned taste aversion than the non-selective amylin analog cagrilintide, and its weight loss was primarily driven by a reduction in fat mass.
Bioactivity
Eloralintide (LY3841136) is a next-generation, selective, long-acting amylin receptor agonist. In vitro studies show that eloralintide preferentially activates the human amylin 1 receptor (AMY1R), with an activation potency for AMY1R that is 12-fold and 11-fold greater than that for the calcitonin receptor (CTR) and the amylin 3 receptor (AMY3R), respectively. Its highly selective design is intended to reduce side effects associated with calcitonin activity and to improve gastrointestinal tolerability.
In vivo research
Eloralintide demonstrated dose-dependent reductions in food intake and body weight in a diet-induced obesity (DIO) rat model.
Animal model: Diet-induced obesity (DIO) rats, lean rats
Dosage: Multiple dose groups (specific doses depend on the study design; potency assessed via ED50)
Administration: Subcutaneous injection, once every 3 days; or once weekly
Results: In DIO rats, eloralintide significantly reduced food intake and body weight (weight loss primarily attributed to reduced fat mass). Its weight-loss potency, food intake suppression, and fat mass reduction were all superior to those of the non-selective amylin analog cagrilintide. Meanwhile, compared with cagrilintide, eloralintide induced significantly less conditioned taste aversion in lean rats (p < 0.05), suggesting better gastrointestinal tolerability.
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