Tecalcet Hydrochloride 是钙敏感受体 (CaSR) 的变构正向调节剂。 Tecalcet Hydrochloride 增加了对细胞外钙离子活化的敏感性。

Tecalcet Hydrochloride is an allosteric and positive modulator of the calcium-sensing receptor(CaSR). Tecalcet Hydrochloride increases the sensitivity to the activation of extracellular Ca2+.

Tecalcet Hydrochloride (0.1-100 nM) shifts the concentration-response curve for extracellular Ca2 to the left and decreases the EC50 value to 0.61 mM. Tecalcet Hydrochloride (0.1-100 μM) increases Ca2+ in a dose-dependent and stereoselective manner[3].

In male Sprague-Dawley rats with renal insufficiency, Tecalcet Hydrochloride (1.5 and 15 mg/kg, oral) inhibits PT cell proliferation and reduces serum PTH level in a dose-dependent manner. Tecalcet Hydrochloride reduces the number of BrdU-positive PT cells by 20% at a low dose (1.5 mg/kg), and by 50% at a high dose (15 mg/kg)[1].

177172-49-5

C18H23Cl2NO

340.29

R-568 hydrochloride;R-568 盐酸盐

DMSO:40 mg/mL (117.5 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years