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Compound 54149

Chemical Structure : Compound 54149

CAS No.: 2866254-56-8

Compound 54149 ((R)-85339)

Catalog No.: PC-21721Not For Human Use, Lab Use Only.

Compound 54149 is novel positive allosteric modulator (PAM) of calcium sensing receptor (CaSR) with EC50 of 41 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Compound 54149 is novel positive allosteric modulator (PAM) of calcium sensing receptor (CaSR) with EC50 of 41 nM.
Compound 54149 stabilizes a distinct active-state CaSR dimer conformation.
Compound 54149 suppresses PTH secretion better than the approved PAM drugs, inhibits PTH secretion dose-dependently (IC50=583 nM) in extracted parathyroid glands from wild-type (WT) C57/BL6 (B6) mice.
Compound 54149 reduces serum PTH at lower doses with less hypocalcemia than cinacalcet and evocalcet.

Physicochemical Properties

M.Wt 326.41
Formula C18H18N2O2S
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

(R)-1-(benzo[d][1,3]dioxol-4-yl)-N-(2-(benzo[d]isothiazol-3-yl)ethyl)ethan-1-amine

References

1. Liu F, et al. bioRxiv. 2023 Dec 27:2023.12.27.573448.

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