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NPS-2143 HCl {[allProObj[0].p_purity_real_show]}

货号:A464000 同义名: SB-262470A hydrochloride;NPS 2143 (hydrochloride)

NPS-2143 HCl (SB-262470A hydrochloride)是一种口服活性的钙感受器拮抗剂,选择性且高效地拮抗钙离子感受器(CaSR)。NPS-2143盐酸盐(SB-262470A盐酸盐)能够阻断在表达人体钙感受器的HEK 293细胞中通过激活钙离子受体引起的细胞内Ca2+浓度增加(IC50=43 nM)。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
NPS-2143 HCl 化学结构 CAS号:324523-20-8
NPS-2143 HCl 化学结构
CAS号:324523-20-8
NPS-2143 HCl 3D分子结构
CAS号:324523-20-8
NPS-2143 HCl 化学结构 CAS号:324523-20-8
NPS-2143 HCl 3D分子结构 CAS号:324523-20-8
规格 价格 会员价 库存 数量
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NPS-2143 HCl 纯度/质量文件 产品仅供科研

货号:A464000 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 CaSR 其他靶点 纯度
NPS-2143 ++++

Ca(2+) receptor, IC50: 43 nM

98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

NPS-2143 HCl 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 fAβ25-35± 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].

NPS-2143 HCl 动物研究

Dose Mice: 45 mg/kg[4] (p.o.); 30 mg/kg[4] (i.p.) Rat: 1 mg/kg[5] (i.v.)
Administration p.o., i.p., i.v.

NPS-2143 HCl 参考文献

[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.

NPS-2143 HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.22mL

11.23mL

2.25mL

1.12mL

22.45mL

4.49mL

2.25mL

NPS-2143 HCl 技术信息

CAS号324523-20-8
分子式C24H26Cl2N2O2
分子量 445.381
别名 SB-262470A hydrochloride;NPS 2143 (hydrochloride);SB-262470A;NPS-2143 hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

DMSO: 105 mg/mL(235.75 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 1.5 mg/mL(3.37 mM),配合低频超声,并水浴加热至45℃助溶

动物实验配方
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