Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Cinacalcet hydrochloride (AMG-073 hydrochloride) is a naphthalene derivative and CALCIMIMETIC AGENT that increases the sensitivity of PARATHYROID GLAND calcium-sensing receptors to serum calcium. This action reduces parathyroid hormone secretion and decreases serum calcium in the treatment of PARATHYROID DISEASES.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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10 mg | 在庫あり | ¥ 10,000 | |||
25 mg | 在庫あり | ¥ 15,000 | |||
50 mg | 在庫あり | ¥ 18,500 | |||
100 mg | 在庫あり | ¥ 34,000 | |||
200 mg | 在庫あり | ¥ 45,000 | |||
500 mg | 在庫あり | ¥ 75,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 11,000 |
説明 | Cinacalcet hydrochloride (AMG-073 hydrochloride) is a naphthalene derivative and CALCIMIMETIC AGENT that increases the sensitivity of PARATHYROID GLAND calcium-sensing receptors to serum calcium. This action reduces parathyroid hormone secretion and decreases serum calcium in the treatment of PARATHYROID DISEASES. |
ターゲット&IC50 | CaSR:2.8 μM(EC50) |
In vitro | Significant dose-dependent reductions in serum calcium levels were observed at 4, 8, and 24 hours post-oral administration of AMG-073 at dosages of 3, 10, and 30 mg/kg. A transient decrease in serum phosphorus levels was noted only with the highest dosage of AMG-073. Oral administration of Cinacalcet HCl at 1, 3, 10, and 30 mg/kg in 20% sulfobutylether-β-cyclodextrin sodium to normal rats induced a significant dose-dependent reduction in PTH levels within 1 to 4 hours. By 8 hours post-dosing, a significant reduction in PTH levels was observed with 10 and 30 mg/kg doses compared to the control group, with this effect dissipating after 24 hours. Additionally, an increase in calcitonin levels accompanying PTH suppression was observed with 40 mg/kg AMG-073 in rats. Similar to normal rats, a rapid dose-dependent reduction in PTH and calcium levels was noted in five out of six nephrectomized rats following oral AMG-073 administration. Furthermore, oral administration of 5 and 10 mg/kg Cinacalcet HCl for 4 weeks significantly reduced the weight of the parathyroid gland compared to the control group. |
In vivo | Cinacalcet HCl induces a concentration-dependent increase in cytoplasmic calcium levels in human embryonic kidney cells expressing the CaSR (Calcium-Sensing Receptor). Furthermore, in bovine parathyroid cells and a buffer containing 0.5 mM calcium, a concentration-dependent decrease in PTH (Parathyroid Hormone) levels was observed when treated with AMG 073 (Cinacalcet) concentrations ranging from 3 nM to 1 μM, achieving an IC50 of 27 nM. |
別名 | AMG-073 HCl, Cinacalcet HCl, AMG-073 hydrochloride, Cinacalcet |
分子量 | 393.87 |
分子式 | C22H23ClF3N |
CAS No. | 364782-34-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (126.95 mM)
You can also refer to dose conversion for different animals. 詳細
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Cinacalcet hydrochloride 364782-34-3 GPCR/G Protein CaSR AMG-073 AMG-073 HCl Endogenous Metabolite Cinacalcet HCl Cinacalcet Hydrochloride Calcium-sensing receptor Inhibitor AMG 073 AMG-073 hydrochloride AMG 073 Hydrochloride AMG073 Hydrochloride AMG-073 Hydrochloride Cinacalcet inhibit AMG073 inhibitor