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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。
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。
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
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
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)
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)
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
Kate E Lines et al.
Journal of molecular endocrinology, 67(3), 83-94 (2021-07-06)
Corticotrophinomas represent 10% of all surgically removed pituitary adenomas, however, current treatment options are often not effective, and there is a need for improved pharmacological treatments. Recently, JQ1+, a bromodomain inhibitor that promotes gene transcription by binding acetylated histone residues
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
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