<生产厂家价格>

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

用途

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

名称

[ CAS 号 ]:
324523-20-8

[ 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

[英文别名 ]:

MFCD16038896
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.

[相关活性小分子]

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 | 依伏卡塞 | 雷尼酸锶 | 钙敏感受体拮抗剂I | SB-423562

物理化学性质

[ 分子式 ]:
C₂₄H₂₆Cl₂N₂O₂

[ 分子量 ]:
445.381

[ 精确质量 ]:
444.137146

[ 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

文献

Acetylcholine protects mesenteric arteries against hypoxia/reoxygenation injury via inhibiting calcium-sensing receptor.

J. Pharmacol. Sci. 127 , 481-8, (2015)

The Ca(2+)-sensing receptor (CaSR) plays an important role in regulating vascular tone. In the present study, we investigated the positive effects of the vagal neurotransmitter acetylcholine by suppre...

Parathyroid-specific deletion of dicer-dependent microRNAs abrogates the response of the parathyroid to acute and chronic hypocalcemia and uremia.

FASEB J. 29 , 3964-76, (2015)

MicroRNAs (miRNAs) down-regulate gene expression and have vital roles in biology but their functions in the parathyroid are unexplored. To study this, we generated parathyroid-specific Dicer1 knockout...

更多文献

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

用途

名称

生物活性

物理化学性质

安全信息

文献

推荐生产厂家/供应商：

热门化合物