产品
编 号：F211987
分子式：C18H23Cl2NO
分子量：340.29
分子式：C18H23Cl2NO
分子量：340.29
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 177172-49-5
产品详情
生物活性：
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 Ca2+.
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.
体外研究：
Tecalcet (NPS 568, 0.1-100 μM) increase [Ca2+]i in a concentrationdependent and stereoselective manner.Tecalcet (NPS 568, 0.1-100 nM) shiftes the concentration-response curve for extracellular Ca2+ to the left without affecting the maximal response and, thereby, decreasesthe EC50 value for extracellular Ca21 to 0.61±0.04 mM.
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 Ca2+.
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.
体外研究：
Tecalcet (NPS 568, 0.1-100 μM) increase [Ca2+]i in a concentrationdependent and stereoselective manner.Tecalcet (NPS 568, 0.1-100 nM) shiftes the concentration-response curve for extracellular Ca2+ to the left without affecting the maximal response and, thereby, decreasesthe EC50 value for extracellular Ca21 to 0.61±0.04 mM.
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