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Product Name: | PCO371 | Synonyms: | PCO371;CPD2050;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-;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-2,4-imidazolidinedione;PCO371,PCO 371,inhibit,Inhibitor,THR,PCO-371,Thyroid Hormone Receptor;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-dimethylimidazolidine-2,4-dione | CAS: | 1613373-33-3 | MF: | C29H32F3N5O6S | MW: | 635.65 | EINECS: | | Product Categories: | | Mol File: | 1613373-33-3.mol | |
| PCO371 Chemical Properties |
density | 1.47±0.1 g/cm3(Predicted) | storage temp. | Store at -20°C | solubility | DMSO: 125 mg/mL (196.65 mM) | pka | 8.39±0.10(Predicted) | InChIKey | LDZJFVOUPUFOHX-UHFFFAOYSA-N | SMILES | C1(=O)N(C2=CC(C)=C(CCS(N3CCC4(N=C(C5=CC=C(OC(F)(F)F)C=C5)NC4=O)CC3)(=O)=O)C(C)=C2)C(C)(C)C(=O)N1 |
| PCO371 Usage And Synthesis |
Description | PCO371 is a novel, orally active small molecule that acts as a full agonist of PTHR1. PCO371 does not affect the PTH type 2 receptor (PTHR2), and analysis using PTHR1-PTHR2 chimeric receptors indicated that Proline 415 of PTHR1 is critical for PCO371-mediated PTHR1 activation[1].
| Biological Activity | PCO371 selectively induces cAMP production in COS-7 cells expressing human PTH1R (EC50 = 2.4 μM) over COS-7 cells expressing human PTH2R (EC50 = > 100 μM). PCO371 (1 and 3 μM) induces calcium release from isolated fetal rat long bones. It increases lumbar spine and proximal femur bone mineral density (BMD), lumbar spine bone strength, serum levels of osteocalcin, and bone formation in the lumbar spine without affecting serum calcium levels in an ovariectomized (OVX) rat model of osteopenia when administered at a dose of 10 mg/kg per day. PCO371 (9 mg/kg) increases serum, but not urinary, calcium levels in a hypocalcemic thyroparathyroidectomized (TPTX) rat model of hypothyroidism. |
| PCO371 Preparation Products And Raw materials |
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