PTH1R Agonist

PTH (1-34) amide human is a type 1 PTH/PTHrP receptor agonist. PTH (1-34) amide human activates adenylate cyclase and phospholipase C pathways, thereby mediating mineral ion homeostasis and bone metabolism regulation. PTH (1-34) amide human increases serum calcium, decreases serum phosphorus, regulates renal excretion, while inducing the inhibition of endogenous PTH (1-84) and the increase of 1,25-dihydroxyvitamin D2 and bone resorption. PTH (1-34) amide human stimulates phosphatidylcholine hydrolysis via phospholipase D mediation, and its hypercalcemic effect is inhibited by human PTH-(7-84). PTH (1-34) amide human can be used in the research of diseases related to humoral hypercalcemia of malignancy.

PTH1R agonist 3 (Example 47) is a parathyroid hormone 1 receptor (PTH1R) agonist with a pEC₅₀ value of less than 6. PTH1R agonist 3 can be used for the study of bone diseases, such as osteoporosis.

PTH1R agonist 2 (example 3) is a parathyroid hormone 1 receptor (PTH1R) agonist. PTH1R agonist 2 can be used for research of hypoparathyroidism and osteoporosis.

PTH1R agonist 1 (Example 2) is a parathyroid hormone 1 receptor (PTH1R) agonist. PTH1R agonist 1 can be used for research of hypoparathyroidism and osteoporosis.

CH5447240 is an orally active agonist of parathyroid hormone receptor 1 (PTHR1). CH5447240 stimulates cAMP production in HKRK-B7 cells expressing hPTHR1, with an EC₅₀ of 12 μM. CH5447240 exhibits PTH-like activity, elevating serum calcium and reducing serum phosphate. CH5447240 can be used for research on hypoparathyroidism.

PTH1R agonist 4 (Example 63) is a parathyroid hormone 1 receptor (PTH1R) agonist with a pEC₅₀ value greater than 7. PTH1R agonist 4 can be used for the study of bone diseases, such as osteoporosis.