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品質等級
化驗
≥98% (HPLC)
形狀
powder
光學活性
[α]20/D +20 to +24°, c = 1.0 in methanol
儲存條件
desiccated
顏色
white to beige
溶解度
DMSO: >10 mg/mL
儲存溫度
2-8°C
SMILES 字串
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 密鑰
ZEBNDUQLNGYBNL-VEIFNGETSA-N
應用
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。
訊號詞
Warning
危險分類
Acute Tox. 4 Dermal - Acute Tox. 4 Inhalation - Acute Tox. 4 Oral - Aquatic Acute 1 - Aquatic Chronic 1
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
其他客户在看
Novel activating mutations of the calcium-sensing receptor: the calcilytic NPS-2143 mitigates excessive signal transduction of mutant receptors
The Journal of Clinical Endocrinology and Metabolism, 95(10), E229-E233 (2010)
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
Archives of Biochemistry and Biophysics, 657, 15-22 (2018)
Progress in Medicinal Chemistry, 57 (2018)
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
Archives of Biochemistry and Biophysics, 640, 10-16 (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)
Endocrinology, 156(9), 3114-3121 (2015)
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