生物活性
NPS-2143 (SB262470) is a selective potent calcium ion-sensing receptor antagonist with IC50 of 43 and 41 nM for cytoplasmic Ca2+concentrations and parathyroid hormone secretion, respectively. NPS-2143 blocks increases in cytoplasmic Ca2+concentrations elicited by human Ca2+ receptors expressed in HEK293 cells . NPS-2143 (SB262470), even at much higher concentrations (3 μM), did not influence the activity of a number of other G protein-coupled receptors, including those most structurally homologous to the Ca2+receptor.NPS-2143 (SB262470) also stimulates parathyroid hormone secretion from bovine parathyroid cells . In addition, administration of NPS-2143 resulted in moderate but sustained increases in plasma PTH levels and marked increases in bone formation and resorption with no net bone gain or loss.
化学数据
| 分子量 | 408.92 |
| 分子式 | C24H25ClN2O2 |
| CAS号 | 284035-33-2 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO 80 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | HEK 293 4.0-7 cells |
| 方法 | On-line continuous measurements of fluorescence in fluo-3- or fura-2-loaded HEK 293 4.0-7 cells are obtained using a custom-built spectrofluorimeter or a fluorescence imaging plate reader instrument. NPS-2143 is incubated with cells for 1 minute before increasing the concentration of extracellular Ca2+ from 1.0 mM to 1.75 mM. NPS-2143 is tested individually at a concentration of 100 μg/mL (20 μM-80 μM) and those causing more than a 40% inhibition of the control response are considered to be biologically active. |
| 浓度 | 20 μM-80 μM |
| 处理时间 | |
| 动物实验 |
|---|
| 动物模型 | Chronic indwelling catheters are implanted in the inferior vena cava and in the abdominal aorta of male Sprague-Dawley rats. |
| 配制 | NPS 2143 is dissolved in 20% aqueous solution of 2-hydroxypropyl-β-cyclodextrin. |
| 剂量 | ≤0.1 μmol/kg · min |
| 给药处理 | Administered via i.v. |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4455 mL | 12.2273 mL | 24.4547 mL |
| 5 mM | 0.4891 mL | 2.4455 mL | 4.8909 mL |
| 10 mM | 0.2445 mL | 1.2227 mL | 2.4455 mL |
m.cnreagent.com