A PTH1R agonist
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PCO371

Item No. 39182

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A solid
Solubility(Learn about Variance in 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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $80

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    5 mg

    $357

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    10 mg

    $634

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    50 mg

    $1,782

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    Product Description

    PCO371 is a parathyroid hormone receptor type 1 (PTH1R) agonist.1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Tamura, T., Noda, H., Joyashiki, E., et al. Identification of an orally active small-molecule PTHR1 agonist for the treatment of hypoparathyroidism. Nat. Commun. 7, 13384 (2016).