PCO371

PCO371 is a parathyroid hormone receptor type 1 (PTH1R) agonist. It 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.Formal Name: 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. CAS Number: 1613373-33-3. Molecular Formula: C29H32F3N5O6S. Formula Weight: 635.7. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Methanol: Soluble. SMILES: O=S(N1CCC2(NC(C3=CC=C(OC(F)(F)F)C=C3)=NC2=O)CC1)(CCC4=C(C)C=C(N5C(C)(C)C(NC5=O)=O)C=C4C)=O. InChi Code: InChI=1S/C29H32F3N5O6S/c1-17-15-20(37-26(40)34-24(38)27(37,3)4)16-18(2)22(17)9-14-44(41,42)36-12-10-28(11-13-36)25(39)33-23(35-28)19-5-7-21(8-6-19)43-29(30,31)32/h5-8,15-16H,9-14H2,1-4H3,(H,33,35,39)(H,34,38,40). InChi Key: LDZJFVOUPUFOHX-UHFFFAOYSA-N.