CTR/AMYR modulator-2 is a dual agonist of human amylin receptor 3 ( AMY3R ) and calcitonin receptor ( CTR ). CTR/AMYR modulator-2 activates AMY3R and CTR, stimulating Rel EC 50 of cAMP production in UMUC3 cells by 4 nM and 1 nM, respectively. CTR/AMYR modulator-2 may be used in research on type 2 diabetes and obesity [1].
In Vitro, CTR/AMYR modulator‑2 (Example 107) acts as an agonist at the human amylin receptor (AMY3R) in UMUC3 cells, with a Rel EC50 of 4 nM and an Emax of 99% as determined in a 20‑point concentration‑response assay following 30 min of incubation[1]. CTR/AMYR modulator‑2 acts as an agonist at the human calcitonin receptor (CTR) in UMUC3 cells, with a Rel EC50 of 1 nM and an Emax of 88% under the same 20‑point assay conditions[1].
References:
[1]. Renato A. BAUER, et al. 4-phenyl-1h-pyrazolo[3,4-b]pyridine-5-carboxamide derivatives as amylin and/or calcitonin receptor agonists for the treatment of type 2 diabetes, obesity or overweight. WO2025240893A1. 2025.
In Vitro, CTR/AMYR modulator‑2 (Example 107) acts as an agonist at the human amylin receptor (AMY3R) in UMUC3 cells, with a Rel EC50 of 4 nM and an Emax of 99% as determined in a 20‑point concentration‑response assay following 30 min of incubation[1]. CTR/AMYR modulator‑2 acts as an agonist at the human calcitonin receptor (CTR) in UMUC3 cells, with a Rel EC50 of 1 nM and an Emax of 88% under the same 20‑point assay conditions[1].
References:
[1]. Renato A. BAUER, et al. 4-phenyl-1h-pyrazolo[3,4-b]pyridine-5-carboxamide derivatives as amylin and/or calcitonin receptor agonists for the treatment of type 2 diabetes, obesity or overweight. WO2025240893A1. 2025.