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PCO371

Chemical Structure : PCO371

CAS No.: 1613373-33-3

PCO371 (PCO-371)

Catalog No.: PC-35256Not For Human Use, Lab Use Only.

PCO371 is a potent, selective, orally active, full agonist of the PTH type 1 receptor (PTHR1) with EC50 of 2.4 uM in cell-based assays, does not affect PTHR2.

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Biological Activity

PCO371 is a potent, selective, orally active, full agonist of the PTH type 1 receptor (PTHR1) with EC50 of 2.4 uM in cell-based assays, does not affect PTHR2.
PCO371 exhibits PTH-like biological activity in osteopenic ovariectomized (OVX) rats and in hypocalcemic thyroparathyroidectomized (TPTX) rats after oral administration.
PCO371 increases bone mineral density (BMD) and bone strength as effectively as PTH by intravenous administration in vivo.
PCO371 fuctions as a Gprotein biased agonist in relative to PTH.

Physicochemical Properties

M.Wt 635.659
Formula C29H32F3N5O6S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Tamura T, et al. Nat Commun. 2016 Nov 18;7:13384.
2. Nishimura Y, et al. J Med Chem. 2020 May 28;63(10):5089-5099.
3. Li-Hua Zhao, et al. Nature. 2023 Jul 31. doi: 10.1038/s41586-023-06467-w.

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