2. GPCR/G Protein
  3. CaSR
  4. NPS-467

NPS-467 是一种钙敏感受体 (CaR) 激活剂和立体特异性试剂，仅其 R-对映体具有活性。NPS-467 可提高 CaR 对细胞外钙激活作用的敏感性。NPS-467 可刺激鳟鱼分泌斯钙素 (STC) 并抑制鳟鱼鳃的钙转运。NPS-467 对鳟鱼的血清降钙素水平无影响。

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NPS-467

NPS-467 Chemical Structure

CAS No. : 148717-47-9

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NPS-467 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NPS-467 is a calcium-sensing receptor (CaR) activator and stereospecific agent with only its R-enantiomer active. NPS-467 increases the sensitivity of the CaR to activation by extracellular calcium. NPS-467 stimulates stanniocalcin (STC) secretion in trout and induces inhibition of gill calcium transport in trout. NPS-467 has no effect on serum calcitonin levels in trout[1].

体内研究
(In Vivo)

NPS-467 (R-对映体) (0.25-2.0 mg/kg；腹腔注射；单次给药) 可对幼龄 rainbow trout 的 STC 分泌产生立体特异性、剂量及时间依赖性的刺激作用，其 ED50 为 0.44 mg/kg，血清 STC 水平最高可升高 9 倍，但对血清 CT 水平无影响[1]。
NPS-467 (R-对映体) (0.25-2.0 mg/kg；腹腔注射；单次给药) 可通过增强 STC 的释放，对幼体虹鳟鱼的鳃钙转运产生立体特异性、剂量依赖性的抑制作用，其 ED50 为 0.5 mg/kg，且该效应可被鱼类 STC 抗血清完全阻断[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Oncorhynchus mykiss (juvenile, 150-250 g)[1]
Dosage: 0.25 mg/kg; 0.5 mg/kg; 1.0 mg/kg; 2.0 mg/kg
Administration: i.p.; single dose
Result: Produced statistically significant stimulatory effects on STC secretion (P < 0.01-0.001).
Raised serum STC levels maximally to 2069 ng/mL, representing a 9-fold induction over controls; the response plateaued at doses above 2.5 mg/kg.
Achieved an ED50 of 0.44 mg/kg for STC secretion stimulation.
Induced a rapid response, with maximal 14-fold STC induction by 0.5 hours post-injection, which persisted for up to 4 hours.
Showed no statistically significant effects on serum CT levels at doses of 0.25, 0.5, 1.0, or 2.0 mg/kg.
Animal Model: Oncorhynchus mykiss (fingerling, 1-2 g)[1]
Dosage: 0.25 mg/kg; 0.5 mg/kg; 1.0 mg/kg; 2.0 mg/kg
Administration: i.p.; single dose
Result: Produced consistent, dose-dependent inhibitory effects on GCAT across three experiments, with statistically significant reductions at all tested doses (P < 0.05-0.01).
Achieved an ED50 of 0.5 mg/kg (2.5 μmol/kg) for GCAT inhibition, which was similar to the ED50 for STC secretion stimulation.
Had its inhibitory effects on GCAT at 2.0 mg/kg completely neutralized by passive immunization with fish STC antiserum, with GCAT rates not significantly different from controls receiving nonimmune rabbit serum alone.
分子量

269.38

Formula

C18H23NO
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

NPS-467 相关分类

  • 摩尔计算器

  • 稀释计算器

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Keywords:

NPS-467148717-47-9NPS467NPS 467CaSRCalcium-sensing receptorcalcium-sensing receptorjuvenile rainbow troutserum calcitoninstanniocalcintroutgill calcium transportextracellular calciumfingerling rainbow troutCaRSTCInhibitorinhibitorinhibit

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目录号：
HY-182543
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