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NPS-2143

CAS No. : 284035-33-2

MCE 站：NPS-2143

产品活性：NPS-2143 (SB-262470A)，口服活性溶钙剂， 是选择性的钙敏感受体 (CaSR) 拮抗剂。NPS-2143 (SB-262470A) 通过激活表达人 Ca²⁺ 受体的 HEK 293 细胞中的 Ca²⁺ 受体而引起的胞浆 Ca²⁺ 浓度增加 (IC₅₀=43 nM)。

研究领域：GPCR/G Protein

作用靶点：CaSR

In Vitro: NPS-2143 (SB-262470A) stimulates parathyroid hormone (PTH) secretion from bovine parathyroid cells with EC₅₀ of 41 nM. Moreover, NPS 214 also blocks the inhibitory effects of calcimimetic NPS R-467 on PTH secretion from bovine parathyroid cells and the inhibitory effects of extracellular Ca²⁺ on isoproterenol-stimulated increases in cyclic AMP formation.
In HEK 293 cells transiently expressing hCaSRs, NPS-2143 significantly suppresses the kokumi taste by effectively inhibiting the activity of both GSH and γ-Glu-Val-Gly.?A recent study shows that NPS-2143 treatment suppresses low molecular weight fractions of azuki hydrolysate-induced cholecystokinin (CCK) secretion in CaSR-transfected HEK 293 cells.

In Vivo: NPS-2143 (SB-262470A) results in a rapid 4- to 5-fold increase in plasma PTH levels and also a transient increase in plasma Ca²⁺?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.

相关产品：Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Orally Active Compound Library  |  Cinacalcet  |  Tecalcet Hydrochloride  |  NPS-2143 hydrochloride  |  Strontium Ranelate  |  Ligustroflavone  |  Calhex 231 hydrochloride  |  Calcium-Sensing Receptor Antagonists I  |  GSK3004774

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