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PCO371 is a novel, orally active small molecule full agonist of PTHR1. PCO371 does not affect the PTH type 2 receptor (PTHR2). Oral administration of PCO371 to osteopenic rats provokes a significant increase in bone turnover with limited increase in bone mass. In hypocalcemic rats, PCO371 restores serum calcium levels without increasing urinary calcium, and with stronger and longer-lasting effects than PTH injections. PCO371 induces cAMP production with an EC50 of 2.4 μM in COS-7 cells expressing hPTHR1, and 2.5 μM in COS-7 cells transfected with hPTHR1-delNT, and also enhances the phospholipase C activity (EC50=17 μM).
| Molecular Weight | 635.65 |
| Formula | C29H32F3N5O6S |
| CAS Number | 1613373-33-3 |
| Form | Solid |
| Solubility (25°C) | DMSO 95 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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