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CAS No.: 324523-20-8

NPS-2143 HCl Catalog No. CSN18211

Synonyms: SB-262470A hydrochloride;SB-262470A HCl;NPS 2143 (hydrochloride)

NPS-2143 HCl is a potent and selective calcium ion-sensing receptor antagonist with IC50 of 43 and 41 nM for cytoplasmic Ca2+ concentrations and parathyroid hormone secretion, respectively.

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400-920-2911

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实验方案

技术信息

生物活性

描述Calcium-sensing receptor (CaSR) is a G-protein coupled receptor expressed on the surface of parathyroid cells that mediates the secretion of parathyroid hormone (PTH). NPS-2143 hydrochloride is an antagonist for CaSR that inhibits the increase of cytoplasmic Ca²⁺ level induced by the activation of CaSR in HEK 293 cells expressing human CaSR with an IC₅₀ value of 43 nM. NPS-2143 hydrochloride also stimulated the secretion of PTH from bovine parathyroid cells with an EC₅₀ value of 41 nM^[1]. In human astrocytes, incubation of NPS-2143 hydrochloride at 100 nM for 30 min inhibited the endogenous secretion of Aβ₄₂/Aβ₄₂-os. The treatment of NPS-2143 hydrochloride also promoted the translocation of hAPP to the plasma membrane in fAβ_25-35± microglial cytokine mixture-exposed astrocytes^[2]. Oral administration of NPS-2143 hydrochloride (100 μmol/kg) for 8 weeks led to a sustained elevation of plasma PTH level and a significant increase of bone turnover in osteopenic ovariectomized (OVX) rats. Daily oral administration of NPS-2143 hydrochloride (100 μmol/kg) for 5 weeks together with the treatment of 17β-estradiol increased cancellous bone area in OVX rats compared to their counterparts administered with 17β-estradiol alone^[1].
作用机制NPS-2143 hydrochloride acts as an CaSR antagonist by binding to the cavity of the transmembrane domains of CaSR, thereby inhibiting its activation^[3].
动物研究
剂量
Mice: 45 mg/kg^[4] (p.o.); 30 mg/kg^[4] (i.p.) Rat: 1 mg/kg^[5] (i.v.)

给药途径
p.o., i.p., i.v.
参考文献

动物研究
剂量	Mice: 45 mg/kg^[4] (p.o.); 30 mg/kg^[4] (i.p.) Rat: 1 mg/kg^[5] (i.v.)
给药途径	p.o., i.p., i.v.

[1] Nemeth EF, Delmar EG, et al. Calcilytic compounds: potent and selective Ca2+ receptor antagonists that stimulate secretion of parathyroid hormone. J Pharmacol Exp Ther. 2001;299(1):323-31.
[2] Chiarini A, Armato U, et al. Calcium-Sensing Receptor Antagonist NPS 2143 Restores Amyloid Precursor Protein Physiological Non-Amyloidogenic Processing in Aβ-Exposed Adult Human Astrocytes. Sci Rep. 2017;7(1):1277.
[3] Petrel C, Kessler A, et al. Positive and negative allosteric modulators of the Ca2+-sensing receptor interact within overlapping but not identical binding sites in the transmembrane domain. J Biol Chem. 2004;279(18):18990-7.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2453 mL
- 11.2264 mL
- 22.4527 mL
- 5 mM
- 0.4491 mL
- 2.2453 mL
- 4.4905 mL
- 10 mM
- 0.2245 mL
- 1.1226 mL
- 2.2453 mL

技术信息

CAS号

324523-20-8

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H26Cl2N2O2

运输

蓝冰

分子量

445.38

别名

SB-262470A hydrochloride;SB-262470A HCl;NPS 2143 (hydrochloride);SB-262470A

溶解度

DMSO	100.0 mg/mL (224.5 mM)

动物实验配方

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