NPS-2143-hydrochloride - CaSR Antagonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENPS-2143 hydrochlorideCat. No.: HY-10171CAS No.: 324523-20-8分式: CHClNO分量: 445.38作靶点: CaSR作通路: GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (224.53 mM)* means solu

2、ble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.2453 mL 11.2264 mL 22.4527 mL5 mM 0.4491 mL 2.2453 mL 4.4905 mL10 mM 0.2245 mL 1.1226 mL 2.2453 mL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，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当

3、天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.61 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.61 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Sm

4、all Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (5.61 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 NPS-2143 hydrochloride是选择性的Ca(2+)受体拮抗剂，IC50为43 nM。户使本产品发表的科研献 Oxid Med Cell Longev. 2017;2017:3869561. Am J Physiol Heart Circ Physiol. 2010 Nov;299(5):H1309-17. Gen Comp Endocrinol. 2018 Oct 1;267

5、:1-8. J Food Sci. 2018 Sep;83(9):2394-2401. J Vet Sci. 2018 Mar 31;19(2):179-187.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Huang Y, Breitwieser GE. Rescue of calcium-sensing receptor mutants by allosteric modulators reveals a conformational checkpoint inreceptor biogenesi

6、s. J Biol Chem. 2007 Mar 30;282(13):9517-252. Marquis, Robert W.; Lago, Amparo M.; Callahan, James F.;Antagonists of the Calcium Receptor. 2. Amino Alcohol-Based ParathyroidHormone Secretagogues. Journal of Medicinal Chemistry (2009), 52(21), 6599-6605.3. Yamamura A, Guo Q, Yamamura H, Zimnicka AM,

7、Pohl NM, Smith KA, Fernandez RA, Zeifman A, Makino A, Dong H, YuanJX.Enhanced Ca2+-sensing receptor function in idiopathic pulmonary arterial hypertension.Circ Res. 2012 Aug 3;111(4):469-81. Epub 2012Jun 22.4. Nakajima S, Hira T, Hara H.Calcium-sensing receptor mediates dietary peptide-induced CCK s

8、ecretion in enteroendocrine STC-1cells.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 biasedsignaling 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 parathyroidhormone. J Pharmacol Exp Ther. 2001 Oct;299(1):323-31.McePdfHeightCaution: Product has not been fully validated for medical ap