NPS-2143 hydrochloride
(Synonyms: 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,NPS2143 hydrochloride;NPS 2143 hydrochloride) 目录号 : GC12240
An orally-active CaSR antagonist
Cas No.:324523-20-8
Sample solution is provided at 25 µL, 10mM.
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NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) blocks increases in cytoplasmic Ca2+ concentrations (IC50=43 nM) elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor[1][2].
NPS-2143 hydrochloride (SB-262470A hydrochloride) stimulates parathyroid hormone (PTH) secretion from bovine parathyroid cells with EC50 of 41 nM. Moreover, NPS-2143 hydrochloride also blocks the inhibitory effects of calcimimetic NPS R-467 on PTH secretion from bovine parathyroid cells and the inhibitory effects of extracellular Ca2+ on isoproterenol-stimulated increases in cyclic AMP formation[1].
When infused intravenously in normal rats, NPS-2143 hydrochloride (SB-262470A hydrochloride) causes a rapid and large increase in plasma levels of PTH. Ca2+ receptor antagonists are termed calcilytics and NPS-2143 is the first substance (either atomic or molecular) shown to possess such activity[1].When administered together with an antiresorptive agent (estradiol), NPS 2143 causes an increase in trabecular bone volume and bone mineral density in osteopenic rats[2].
References:
[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.
| Cas No. | 324523-20-8 | SDF | |
| 别名 | 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,NPS2143 hydrochloride;NPS 2143 hydrochloride | ||
| 化学名 | 2-chloro-6-[(2R)-2-hydroxy-3-[(2-methyl-1-naphthalen-2-ylpropan-2-yl)amino]propoxy]benzonitrile;hydrochloride | ||
| Canonical SMILES | CC(C)(CC1=CC2=CC=CC=C2C=C1)NCC(COC3=C(C(=CC=C3)Cl)C#N)O.Cl | ||
| 分子式 | C24H26Cl2N2O2 | 分子量 | 445.38 |
| 溶解度 | ≥ 44.5 mg/mL in DMSO, ≥ 11.43 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet