| Description | PCO371 (2,4-Imidazolidinedione, 1-(3,5-dimethyl-4-(2-((4-oxo-2-(4-(trifluoromethoxy)phenyl)-1,3,8-triazaspiro(4.5)dec-1-en-8-yl)sulfonyl)ethyl)phenyl)-5,5-dimethyl-) is an orally active full agonist of parathyroid hormone receptor 1. It has no effect on PTH type 2 receptor. |
| In vitro | 在表达hPTHR1的COS-7细胞中，PCO371引发cAMP产生（EC50：2.4μM）。在转染有hPTHR1-delNT的COS-7细胞中，2.5μM的PCO371同样能增强磷脂酶C活性（EC50，17μM）[1]。 |
| Synonyms | 2,4-Imidazolidinedione, 1-(3,5-dimethyl-4-(2-((4-oxo-2-(4-(trifluoromethoxy)phenyl)-1,3,8-triazaspiro(4.5)dec-1-en-8-yl)sulfonyl)ethyl)phenyl)-5,5-dimethyl- |
| molecular weight | 635.65 |
| Molecular formula | C29H32F3N5O6S |
| CAS | 1613373-33-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 120 mg/mL (188.78 mM), Sonication is recommended. |
| References | 1. Tamura T, et al. Identification of an orally active small-molecule PTHR1 agonist for the treatment of hypoparathyroidism. Nat Commun. 2016 Nov 18;7:13384. |