Compound 54149 | CaSR agonist | Probechem Biochemicals

Chemical Structure : Compound 54149

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Compound 54149 (CaSR agonist 54149, (R)-85339)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	326.41
分子式	C18H18N2O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

1. Liu F, et al. bioRxiv. 2023 Dec 27:2023.12.27.573448.
2. Liu F, et al. Science. 2024 Sep 20;385(6715):eado1868.

Compound 54149 (CaSR agonist 54149, (R)-85339)

生物&药学活性

物理化学性质&存储条件

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Compound 54149 (CaSR agonist 54149, (R)-85339)

生物&药学活性

物理化学性质&存储条件

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