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Merck
CN

SML0362

NPS2143 盐酸盐

≥98% (HPLC), Calcium-sensing receptor antagonist, powder

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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关于此项目

经验公式(希尔记法):
C24H25ClN2O2 · HCl
化学文摘社编号:
分子量:
445.38
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
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产品名称

NPS2143 盐酸盐, ≥98% (HPLC)

SMILES string

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

assay

≥98% (HPLC)

form

powder

optical activity

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

storage condition

desiccated

color

white to beige

solubility

DMSO: >10 mg/mL

storage temp.

2-8°C

Quality Level

Application

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。

Biochem/physiol Actions

NPS2143是一种选择性钙敏感受体(CaR)拮抗剂。
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。

pictograms

Exclamation markEnvironment

signalword

Warning

Hazard Classifications

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

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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A Forward Genetic Screen in Zebrafish Identifies the G-Protein-Coupled Receptor CaSR as a Modulator of Sensorimotor Decision Making
Jain RA, et al.
Current Biology, 28(9), 1357-1369 (2018)
Fen-Fen Liu et al.
Cardiorenal medicine (2022-10-11)
Introduction Apoptosis of vascular smooth muscle cells induced by hyperphosphatemia is a critical mechanism of chronic kidney disease-related vascular disorders. The present study investigated whether extracellular calcium-sensing receptor (CaSR) regulates stanniocalcin 2 (STC2) expression in HAoSMCs in vitro and whether
The calcilytic agent NPS 2143 rectifies hypocalcemia in a mouse model with an activating calcium-sensing receptor (CaSR) mutation: relevance to autosomal dominant hypocalcemia type 1 (ADH1)
Hannan FM, et al.
Endocrinology, 156(9), 3114-3121 (2015)
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)

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