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Synonyms | Mimpara, Sensipar,AMG-073 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C22H22F3N.HCl |
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分子量 | 393.87 | CAS No. | 364782-34-3 | ||||
Solubility (25°C)* | 体外 | DMSO | 79 mg/mL (200.57 mM) | ||||
Ethanol | 79 mg/mL (200.57 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Cinacalcet (Mimpara, Sensipar,AMG-073) HCl represents a new class of compounds for the treatment of hyperparathyroidism. |
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in vitro | 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. [2] |
in vivo | 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. [2] |
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Data from [Data independently produced by , , J Bone Miner Res, 2018, doi:10.1002/jbmr.3643]
Data from [Data independently produced by , , Oncotarget, 2016, 7(13):16112-29]
Data from [Data independently produced by , , Biochim Biophys Acta Mol Basis Dis, 2018, 1864(11):3585-3594]
AC-265347 Inhibits Neuroblastoma Tumor Growth by Induction of Differentiation without Causing Hypocalcemia [ Int J Mol Sci, 2022, 23(8)4323] | PubMed: 35457141 |
Calcium-Sensing Receptor in Adipose Tissue: Possible Association with Obesity-Related Elevated Autophagy [ Int J Mol Sci, 2020, 21(20)E7617] | PubMed: 33076271 |
Calcium sensing receptor activation in THP-1 macrophages triggers NLRP3 inflammasome and human preadipose cell inflammation. [ Mol Cell Endocrinol, 2020, 501:110654] | PubMed: 31734269 |
Autophagy mediates calcium-sensing receptor-induced TNFα production in human preadipocytes [Mattar P Biochim Biophys Acta Mol Basis Dis, 2018, 1864(11):3585-3594] | PubMed: 30251678 |
Prevention of Injury-Induced Osteoarthritis in Rodent Temporomandibular Joint by Targeting Chondrocyte CaSR [Zhang M J Bone Miner Res, 2018, 10.1002/jbmr.3643] | PubMed: 30496623 |
Cinacalcet inhibits neuroblastoma tumor growth and upregulates cancer-testis antigens. [Rodríguez-Hernández CJ, et al. Oncotarget, 2016, 7(13):16112-29] | PubMed: 26893368 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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