Tecalcet Hydrochloride (R 568 Hydrochloride), an orally active calcimimetic compound, allosterically and positively modulates the calcium-sensing receptor (CaSR). Tecalcet Hydrochloride (R 568 Hydrochloride) increases the sensitivity to activation by extracellular Ca.
体外研究
Tecalcet (NPS 568, 0.1-100 μM) increase [Ca]i in a concentrationdependent and stereoselective manner.
Tecalcet (NPS 568, 0.1-100 nM) shiftes the concentration-response curve for extracellular Ca to the left without affecting the maximal response and, thereby, decreases
the EC50 value for extracellular Ca21 to 0.61±0.04 mM.
体内研究
Tecalcet (1.5 and 15 mg/kg, orally, twice daily for 4 days) inhibits PT cell proliferation in rats with renal insufficiency.
Animal Model:
10-wk-old Male Sprague-Dawley rats weighing 310-350 g.
Dosage:
1.5 and 15 mg/kg.
Administration:
Orally twice daily for 4 days.
Result:
Did not significantly change serum 1,25 (OH)2D3 levels. In contrast, serum PTH levels were reduced by in a dose-dependent manner.
Clearly reduced the number of BrdU-positive PT cells by 20% at a low dose (1.5 mg/kg body wt), and by 50% at a high dose (15 mg/kg body wt), indicating an antiproliferative effect on PT cells.
Reduced PT cell volume in a dose-dependent manner.
分子式
C18H23Cl2NO
分子量
340.29
CAS号
177172-49-5
运输条件
Room temperature in continental US; may vary elsewhere.