PCO371

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PCO371 是一种有效的、选择性的、口服活性的 PTH 1 型受体 (PTHR1) 完全激动剂，在基于细胞的测定中 EC50 为 2.4 uM。

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; exhibits PTH-like biological activity in osteopenic ovariectomized (OVX) rats and in hypocalcemic thyroparathyroidectomized (TPTX) rats after oral administration; increases bone mineral density (BMD) and bone strength as effectively as PTH by intravenous administration in vivo.Hyperparathyroidism Phase 1 Clinical.

PCO371 is an orally active full agonist of parathyroid hormone receptor 1 (PTHR1), with no effect on PTH type 2 receptor. 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).

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PCO-371

GPCR/G Protein

PTH Receptor

PTH Receptor

Endocrinology

Hyperparathyroidism

1613373-33-3

635.659

C29H32F3N5O6S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (157.32 mM)

O=C1NC(C(C)(C)N1C2=CC(C)=C(CCS(=O)(N(CC3)CCC3(N=C(C4=CC=C(OC(F)(F)F)C=C4)N5)C5=O)=O)C(C)=C2)=O

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

(-20℃)

With Ice Pack

≥ 2 years