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| 品牌 | absin | CAS | 364782-34-3 |
|---|---|---|---|
| 分子式 | C22H23ClF3N | 纯度 | 99% |
| 分子量 | 393.87 | 货号 | abs47028036 |
| 规格 | 100mg | 供货周期 | 现货 |
| 主要用途 | is an orally active, | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Cinacalcet hydrochloride 364782-34-3
| 产品描述 | |
| 描述 | Cinacalcet hydrochloride (AMG-073) is an orally active, second-generation calcimimetic compound; AMG 073 represents a new class of compounds for the treatment of hyperparathyroidism. |
| 纯度 | 99% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 可溶性/溶解性 | Ethanol：33mg/mL(83.78mM) DMSO：79 mg/mL (200.57 mM) |
| 生物活性 | |
| 靶点 | CaSR |
| In vitro(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. |
| In vivo(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. |
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| 研究领域 | |
| 研究领域 | MetabolismPathways and ProcessesCofactors, Vitamins / mineralsVitamins / minerals NeuroscienceProcesses NeuroscienceNeurotransmissionReceptors / ChannelsGPCRGlutamate Receptors Signal TransductionCytoskeleton / ECMExtracellular MatrixStructuresBone Signal TransductionGrowth Factors/HormonesHormones Signal TransductionMetabolismVitamins / Minerals Signal TransductionSignaling PathwayCalcium SignalingOther Signal TransductionSignaling PathwayG Protein SignalingGPCR Signal TransductionSignaling PathwayLipid SignalingPLC Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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