2-氯-6-[(2R)-3-[[1,1-二甲基-2-(2-萘基)乙基]氨基]-2-羟基丙氧基]苯腈盐酸盐

• 常用名: 2-氯-6-[(2R)-3-[[1,1-二甲基-2-(2-萘基)乙基]氨基]-2-羟基丙氧基]苯腈盐酸盐
• 英文名: NPS-2143 hydrochloride
• CAS号: 324523-20-8
• 分子量: 445.381
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₄H₂₆Cl₂N₂O₂
• 熔点: N/A
• 闪点: N/A
• 符号: GHS07, GHS09
• 信号词: Warning

用途

NPS-2143(SB 262470A)是选择性的Ca(2+)受体拮抗剂,IC50为43 nM。

名称

• 中文名: 2-氯-6-[(2R)-3-[[1,1-二甲基-2-(2-萘基)乙基]氨基]-2-羟基丙氧基]苯腈盐酸盐
• 英文名: NPS-2143 hydrochloride

生物活性

• 描述: NPS-2143(SB 262470A)是选择性的Ca(2+)受体拮抗剂,IC50为43 nM。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> CaSR的
  研究领域 >> 代谢疾病
• 参考文献:

  [1]. Huang Y, Breitwieser GE. Rescue of calcium-sensing receptor mutants by allosteric modulators reveals a conformational checkpoint in receptor biogenesis. J Biol Chem. 2007 Mar 30;282(13):9517-25

  [2]. Marquis, Robert W.; Lago, Amparo M.; Callahan, James F.;Antagonists of the Calcium Receptor. 2. Amino Alcohol-Based Parathyroid Hormone Secretagogues. Journal of Medicinal Chemistry (2009), 52(21), 6599-6605.

  [3]. Yamamura A, Guo Q, Yamamura H, Zimnicka AM, Pohl NM, Smith KA, Fernandez RA, Zeifman A, Makino A, Dong H, Yuan JX.Enhanced Ca2+-sensing receptor function in idiopathic pulmonary arterial hypertension.Circ Res. 2012 Aug 3;111(4):469-81. Epub 2012 Jun 22.

  [4]. Nakajima S, Hira T, Hara H.Calcium-sensing receptor mediates dietary peptide-induced CCK secretion in enteroendocrine STC-1 cells.Mol Nutr Food Res. 2012 May;56(5):753-60.

  [5]. Davey AE, Leach K, Valant C, Conigrave AD, Sexton PM, Christopoulos A.Positive and negative allosteric modulators promote biased signaling at the calcium-sensing receptor.Endocrinology. 2012 Mar;153(3):1232-41. Epub 2011 Dec 30.

  [6]. Nemeth EF, et al. Calcilytic compounds: potent and selective Ca2+ receptor antagonists that stimulate secretion of parathyroid hormone. J Pharmacol Exp Ther. 2001 Oct;299(1):323-31.

物理化学性质

• 分子式: C₂₄H₂₆Cl₂N₂O₂
• 分子量: 445.381
• 精确质量: 444.137146
• InChIKey: ZEBNDUQLNGYBNL-VEIFNGETSA-N
• SMILES: CC(C)(Cc1ccc2ccccc2c1)NCC(O)COc1cccc(Cl)c1C#N.Cl
• 储存条件: 2-8°C

安全信息

• 符号: GHS07, GHS09
• 信号词: Warning
• 危害声明: H302 + H312 + H332-H410
• 警示性声明: P273-P280-P501
• 危害码 (欧洲): Xn,N
• 风险声明 (欧洲): 20/21/22-50/53
• 安全声明 (欧洲): 36/37-60-61
• 危险品运输编码: UN 3077 9 / PGIII

靶点实验

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英文别名

• MFCD16038896
• Benzonitrile, 2-chloro-6-[(2R)-3-[[1,1-dimethyl-2-(2-naphthalenyl)ethyl]amino]-2-hydroxypropoxy]-, hydrochloride (1:1)
• 2-Chloro-6-[(2R)-2-hydroxy-3-{[2-methyl-1-(2-naphthyl)-2-propanyl]amino}propoxy]benzonitrile hydrochloride (1:1)
• NPS-2143 (hydrochloride)