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当前位置: 首页 > 信号通路研究 > CaSR > Cinacalcet HCl,AMG073
Cinacalcet HCl,AMG073
Cinacalcet HCl,AMG073
Cinacalcet HCl,AMG073
商品货号:MB5964
CAS 号:364782-34-3
英文名字:盐酸西那卡塞;盐酸甲状旁腺激素
质量标准:>99%,BR
分子式:C22H22F3N.HCl
  • 包装规格:
    规格 库存 发货时间
    100MG [¥680.00]15 现货
    1G [¥2800.00]15 现货,一周内发货
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    商品信息

    质检证书(coa)

    说明书下载

     盐酸西那卡塞;盐酸甲状旁腺激素

    分子式:C22H22F3N.HCl    分子量:393.88

    相关谱图:

    HNMR | HPLC

    产品描述

    AMG-073 HCl (Cinacalcet HCl) 是一种新型化合物,用于治疗甲状旁腺功能亢进。

    靶点

    calcium-sensing receptor

             

    IC50

    2.8 μM

             

    体外研究

    AMG-073 represents a new class of compounds for the treatment of hyperparathyroidism known as calcimimetics, which reduce parathyroid hormone (PTH) synthesis and secretion by increasing the sensitivity of the parathyroid calcium-sensing receptor (CaR) to extracellular calcium. AMG-073 has potential advantages as a therapy for secondary hyperparathyroidism because it mimics the effects of extracellular calcium to suppress PTH secretion, even in the presence of hyperphosphatemia, without the risk of causing hypercalcemia and/or hyperphosphatemia. AMG-073 produces a concentration-dependent increase in cytoplasmic calcium in human embryonic kidney cells expressing the CaSR. In bovine parathyroid cells and a buffer containing calcium 0.5 mM, AMG 073 (3 nM – 1 μM) produces a concentration-dependent decrease in PTH levels with IC50 of 27 nM.

    体内研究

    AMG-073 orally administrated to normal rats at dose of 1, 3, 10, and 30 mg/kg in 20% sulfobutyl ether β-cyclodextrin sodium produces a significant dose-dependent reduction in PTH levels for 1 to 4 hours after administration. At 8 hours, the 10- and 30-mg/kg doses of AMG-073 produces significant reductions in PTH levels compared with controls that disappears by 24 hours. Significant dose-dependent reduction in serum calcium levels are observed at 4, 8, and 24 hours after oral administration of AMG-073 3, 10, and 30 mg/kg, respectively. A transient reduction in serum phosphorus levels is observed only with the highest dose of AMG-073. In addition, increased calcitonin levels that paralleled PTH suppression are observed with AMG-073 40 mg/kg in rats. As in normal rats, a rapid dose-dependent reduction in PTH and calcium levels is observed in 5 of 6 nephrectomized rats after oral administration of AMG-073. In addition, oral AMG-073 at 5 and 10 mg/kg for 4 weeks significantly reduces parathyroid weight compared with controls.

    溶解性

    DMSO 79 mg/mL,水 1 mg/mL,乙醇 33 mg/mL

    稳定性

    2 -20°C粉状,6-80°C溶于DMSO

    特征

           

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