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Merck
CN

SML0362

Sigma-Aldrich

NPS2143 盐酸盐

≥98% (HPLC)

别名:

2-氯-6-[(2R)-3-[[1,1-二甲基-2-(2-萘基)乙基]氨基]-2-羟基丙氧基]-苄腈盐酸盐(1:1), NPS-2143 盐酸盐, SB-262470-A 盐酸盐

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About This Item

经验公式(希尔记法):
C24H25ClN2O2 · HCl
分子量:
445.38
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

方案

≥98% (HPLC)

表单

powder

旋光性

[α]20/D +20 to +24°, c = 1.0 in methanol

储存条件

desiccated

颜色

white to beige

溶解性

DMSO: >10 mg/mL

储存温度

2-8°C

SMILES字符串

Cl.CC(C)(Cc1ccc2ccccc2c1)NC[C@@H](O)COc3cccc(Cl)c3C#N

InChI

1S/C24H25ClN2O2.ClH/c1-24(2,13-17-10-11-18-6-3-4-7-19(18)12-17)27-15-20(28)16-29-23-9-5-8-22(25)21(23)14-26;/h3-12,20,27-28H,13,15-16H2,1-2H3;1H/t20-;/m1./s1

InChI key

ZEBNDUQLNGYBNL-VEIFNGETSA-N

应用

NPS2143盐酸盐已用于研究钙敏感受体的功能:
  • 调节肠钙转运
  • 调节肠钙吸收的局部负反馈
  • 发育过程中的感觉运动决策。

生化/生理作用

NPS2143是一种选择性钙敏感受体(CaR)拮抗剂。该化合物可阻断细胞质钙浓度的增加,IC50为43 nM,并在广泛的细胞外钙浓度范围内刺激牛甲状旁腺细胞分泌甲状旁腺激素(PTH)。
NPS2143是苯烷基胺钙化化合物,可用于治疗常染色体显性低钙血症。它可作为hERG(人类ether-a-go-go相关基因)通道、CYP2D6(细胞色素P450 2D6)和单胺转运蛋白的阻断剂。

象形图

Exclamation markEnvironment

警示用语:

Warning

危险分类

Acute Tox. 4 Dermal - Acute Tox. 4 Inhalation - Acute Tox. 4 Oral - Aquatic Acute 1 - Aquatic Chronic 1

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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分析证书(COA)

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访问文档库

Activation of calcium-sensing receptor by allosteric agonists cinacalcet and AC-265347 abolishes the 1, 25 (OH) 2D3-induced Ca2+ transport: Evidence that explains how the intestine prevents excessive Ca2+ absorption
Wongdee K, et al.
Archives of Biochemistry and Biophysics, 657, 15-22 (2018)
Progress in Medicinal Chemistry, 57 (2018)
Novel activating mutations of the calcium-sensing receptor: the calcilytic NPS-2143 mitigates excessive signal transduction of mutant receptors
Letz S, et al.
The Journal of Clinical Endocrinology and Metabolism, 95(10), E229-E233 (2010)
Hyunji Cho et al.
International journal of molecular sciences, 22(1) (2021-01-06)
Near the bone remodeling compartments (BRC), extracellular calcium concentration (Ca2+o) is locally elevated and bone marrow stromal cells (BMSCs) close to the BRC can be exposed to high calcium concentration. The calcium-sensing receptor (CaSR) is known to play a key
Prolonged exposure to 1, 25 (OH) 2D3 and high ionized calcium induces FGF-23 production in intestinal epithelium-like Caco-2 monolayer: A local negative feedback for preventing excessive calcium transport
Rodrat M, et al.
Archives of Biochemistry and Biophysics, 640, 10-16 (2018)

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