产品描述: NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca2+ concentrations (IC50=43 nM) elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor |
靶点:
IC50: 43 nM (Ca2+ receptor);CalciumChannel;CaSR |
体内研究:
NPS-2143 (SB-262470A) results in a rapid 4- to 5-fold increase in plasma PTH levels in rats. In normotensive rats, NPS-2143 administration (1 mg/kg, i.v.) markedly increases mean arterial blood pressure (MAP) in the presence of parathyroid glands. |
参考文献:
1. Nemeth EF, et al. Calcilytic compounds: potent and selective Ca2+ receptor antagonists that stimulate secretion of parathyroid hormone. J Pharmacol Exp Ther. 2001 Oct;299(1):323-31. 2. Rybczynska A, et al. Hypertensive effect of calcilytic NPS 2143 administration in rats. J Endocrinol. 2006 Oct;191(1):189-95. 3. Ohsu T, et al. Involvement of the calcium-sensing receptor in human taste perception. J Biol Chem. 2010 Jan 8;285(2):1016-22 4. Nakajima S, et al. Calcium-sensing receptor mediates dietary peptide-induced CCK secretion in enteroendocrine STC-1 cells. Mol Nutr Food Res. 2012 May;56(5):753-60 5. Sun J, et al. Calcium-sensing receptor: a sensor and mediator of ischemic preconditioning in the heart. Am J Physiol Heart Circ Physiol. 2010 Nov;299(5):H1309-17. |
溶解性:
DMSO : 17.86 mg/mL (43.68 mM; ultrasonic and adjust pH to 2 with H2O) |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
2.445 ml |
12.227 ml |
24.454 ml |
5 mM |
0.489 ml |
2.445 ml |
4.891 ml |
10 mM |
0.245 ml |
1.223 ml |
2.445 ml |
50 mM |
0.049 ml |
0.245 ml |
0.489 ml |
|
注意: |
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