NPS-2143
Based on 30 publication(s) in Google Scholar
NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca2+ concentrations (IC50=43 nM) elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.94%
- CAS. Nr.: 284035-33-2
- Formel: C24H25ClN2O2
- Molecular Weight:408.92
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) NPS-2143
More- Int J Biol Sci. 2024 Jul 15;20(10):3892-3910. [Abstract]
- Food Chem. 2024 Oct 10;464(Pt 1):141569. [Abstract]
- Phytomedicine. 2021 Apr:84:153507. [Abstract]
- J Agric Food Chem. 2025 Apr 25. [Abstract]
- Int J Mol Med. 2021 Jan;47(1):302-314. [Abstract]
- Acta Physiol. 2026 Jan;242(1):e70142. [Abstract]
- Acta Physiol. 2023 Apr;237(4):e13926. [Abstract]
- Food Funct. 2025 Mar 26. [Abstract]
- Food Funct. 2022 Jun 6;13(11):6233-6243. [Abstract]
- J Clin Endocrinol Metab. 2024 Oct 16:dgae735. [Abstract]
- Int J Mol Sci. 2023 Mar 3;24(5):4921. [Abstract]
- Front Pharmacol. 2022 Feb 23;13:816133. [Abstract]
- Bioorg Chem. 2025 Dec 21:169:109418. [Abstract]
- Am J Physiol Heart Circ Physiol. 2010 Nov;299(5):H1309-17. [Abstract]
- Sci Rep. 2025 May 9;15(1):16209. [Abstract]
- Sci Rep. 2019 Dec 12;9(1):18979. [Abstract]
- J Food Sci. 2018 Sep;83(9):2394-2401. [Abstract]
- J Tradit Complement Med. 2024 Jul 2;15(5):495-508. [Abstract]
- Photochem Photobiol. 2022 Sep;98(5):1157-1166. [Abstract]
- PeerJ. 2026 Jan 5:14:e20546. [Abstract]
- Toxicon. 2026 Jan:269:108660. [Abstract]
- FEBS Open Bio. 2025 Oct 13. [Abstract]
- FASEB Bioadv. 2025 Sep 3;7(8):e70045. [Abstract]
- Neurosci Lett. 2025 Aug 9:865:138351. [Abstract]
- Gen Comp Endocrinol. 2018 Oct 1:267:1-8. [Abstract]
- J Vet Sci. 2018 Mar 31;19(2):179-187. [Abstract]
- University of Verona. 2025.
- University of Verona. 2025.
- Oxid Med Cell Longev. 2021 Jan 12;2021:3010548. [Abstract]
- Oxid Med Cell Longev. 2017:2017:3869561. [Abstract]
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Biologische Aktivität
IC50: 43 nM (Ca2+ receptor)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.46 μM
Compound: 3, NPS 2143
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Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
Activity at rat CaSR in CHO cells assessed as inhibition of calcium ion-induced [3H]inositol phosphate accumulation
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[PMID: 16913701] |
| HEK293 | IC50 |
0.003 nM
Compound: 3
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Displacement of [3H](2-(2-hydroxyphenyl)-6-methyl-5-(2-methylpropyl)-3-(2-phenylethyl)-4(3H)-pyrimidinone) from human calcium receptor expressed in human HEK293 4.0-7 cells by liquid scintillation counting
Displacement of [3H](2-(2-hydroxyphenyl)-6-methyl-5-(2-methylpropyl)-3-(2-phenylethyl)-4(3H)-pyrimidinone) from human calcium receptor expressed in human HEK293 4.0-7 cells by liquid scintillation counting
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[PMID: 19821575] |
| HEK293 | IC50 |
0.043 μM
Compound: NPS-2143
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Inhibitory concentration against human calcium receptor expressed in HEK 293 cells
Inhibitory concentration against human calcium receptor expressed in HEK 293 cells
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[PMID: 15745796] |
| HEK293 | IC50 |
0.058 nM
Compound: 3
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Antagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assay
Antagonist activity at human calcium receptor expressed in HEK293 4.0-7 cells assessed as inhibition of intracellular calcium release by FLIPR assay
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[PMID: 19821575] |
| HEK293 | IC50 |
0.08 μM
Compound: NPS-2143
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Inhibitory concentration for the inhibition of intracellular [Ca2+] release in HEK cells by using FLIPR technology
Inhibitory concentration for the inhibition of intracellular [Ca2+] release in HEK cells by using FLIPR technology
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[PMID: 15686947] |
| HEK293 | IC50 |
23 nM
Compound: NPS-2143
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Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
Negative allosteric modulator activity at human recombinant calcium sensing receptor expressed in HEK cells
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[PMID: 19442519] |
| HEK293 | IC50 |
43 nM
Compound: 27, NPS2143
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Inhibition of human CaSR expressed in HEK293 cells
Inhibition of human CaSR expressed in HEK293 cells
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[PMID: 20218623] |
| PC-12 | IC50 |
0.026 μM
Compound: NPS-2143
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Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
Antagonist activity at human CaSR expressed in rat PC12 cells transfected with zif promoter/luciferase by reporter gene assay
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[PMID: 20472433] |
| TT | IC50 |
0.05 μM
Compound: 1, NPS-2143
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Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
Inhibition of intracellular calcium release in human TT cells containing calcium-sensing receptor by FLIPR
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[PMID: 16216508] |
NPS-2143 (SB-262470A) stimulates parathyroid hormone (PTH) secretion from bovine parathyroid cells with EC50 of 41 nM. Moreover, NPS 214 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].
In HEK 293 cells transiently expressing hCaSRs, NPS-2143 significantly suppresses the kokumi taste by effectively inhibiting the activity of both GSH and γ-Glu-Val-Gly[3]. NPS-2143 treatment suppresses low molecular weight fractions of azuki hydrolysate-induced cholecystokinin (CCK) secretion in CaSR-transfected HEK 293 cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In normotensive rats, NPS-2143 administration (1 mg/kg, i.v.) markedly increases mean arterial blood pressure (MAP) in the presence of parathyroid glands[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 284035-33-2
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Appearance Solid
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Molecular Weight 408.92
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Formel C24H25ClN2O2
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Color White to off-white
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SMILES
N#CC1=C(OC[C@@H](CNC(C)(CC2=CC=C3C=CC=CC3=C2)C)O)C=CC=C1Cl
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Synonyms
SB-262470A
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (30)
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Journal Impact Factor
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Most Recent
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Int J Biol Sci
The Interaction of Calcium-Sensing Receptor with KIF11 Enhances Cisplatin Resistance in Lung Adenocarcinoma via BRCA1/cyclin B1 pathway. [Abstract]2024 Jul 15;20(10):3892-3910. PMID: 39113697 -
Food Chem
Targeted discovery of pea protein-derived GLP-1-secreting peptides by CaSR activation-based molecular docking and their digestive stability. [Abstract]2024 Oct 10;464(Pt 1):141569. PMID: 39418954 -
Phytomedicine
Matrine, as a CaSR agonist promotes intestinal GLP-1 secretion and improves insulin resistance in diabetes mellitus. [Abstract]2021 Apr:84:153507. PMID: 33636577 -
J Agric Food Chem
Novel Cholecystokinin Secretion-Stimulating Peptides from Oat Protein Hydrolysate: Sequence Identification and Insight into the Mechanism of Action. [Abstract]2025 Apr 25. PMID: 40275796 -
Int J Mol Med
Astragaloside IV attenuates cerebral ischemia‑reperfusion injury in rats through the inhibition of calcium‑sensing receptor‑mediated apoptosis. [Abstract]2021 Jan;47(1):302-314. PMID: 33416112 -
Acta Physiol
Upregulated Calcium Sensing Receptor Mediates Pulmonary Venous Remodeling in Pulmonary Hypertension. [Abstract]2026 Jan;242(1):e70142. PMID: 41387174 -
Acta Physiol
2023 Apr;237(4):e13926. PMID: 36606511 -
Food Funct
Bioactive peptides from barley protein hydrolysate stimulate cholecystokinin secretion via calcium-sensing receptor signaling in enteroendocrine cells. [Abstract]2025 Mar 26. PMID: 40134323 -
Food Funct
Digestion characteristics of quinoa, barley and mungbean proteins and the effects of their simulated gastrointestinal digests on CCK secretion in enteroendocrine STC-1 cells. [Abstract]2022 Jun 6;13(11):6233-6243. PMID: 35587126 -
J Clin Endocrinol Metab
Heterogenous Origins of Calcium Homeostasis Disorders Arising from Five Heterozygous Calcium-Sensing Receptor Variants. [Abstract]2024 Oct 16:dgae735. PMID: 39413244 -
Int J Mol Sci
The CaSR Modulator NPS-2143 Reduced UV-Induced DNA Damage in Skh:hr1 Hairless Mice but Minimally Inhibited Skin Tumours. [Abstract]2023 Mar 3;24(5):4921. PMID: 36902353 -
Front Pharmacol
Ca2+-Permeable Channels/Ca2+ Signaling in the Regulation of Ileal Na+/Gln Co-Transport in Mice. [Abstract]2022 Feb 23;13:816133. PMID: 35281933 -
Bioorg Chem
L-tetrahydropalmatine attenuates methamphetamine-induced pulmonary vascular remodeling via CaSR-BMP2/mTOR signaling. [Abstract]2025 Dec 21:169:109418. PMID: 41443015 -
Am J Physiol Heart Circ Physiol
Calcium-sensing receptor: a sensor and mediator of ischemic preconditioning in the heart. [Abstract]2010 Nov;299(5):H1309-17. PMID: 20833954
NPS-2143 purchased from MedChemExpress. Usage Cited in: Am J Physiol Heart Circ Physiol. 2010 Nov;299(5):H1309-17. [Abstract]
Distribution of cardioprotective signaling kinases among fractions prepared from perfusion, IPC, and NPS2143-treated IPC hearts. After nondetergent caveolae fractionation via sucrose gradient ultracentrifugation, equal volume of each collected sucrose fraction is subjected to 4–12% SDS-PAGE under reducing condition and followed with p-ERK1/2 (A), p-AKT (B), and p-GSK-3β (C) IB detection. The representative IBs are taken and shown from one out of three independent experiments.
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Sci Rep
NPS-2143 suppresses malignant phenotypes of retinoblastoma cells involved in regulating NF-κB pathway. [Abstract]2025 May 9;15(1):16209. PMID: 40346093 -
Sci Rep
Shape-dependent toxicity and mineralization of hydroxyapatite nanoparticles in A7R5 aortic smooth muscle cells. [Abstract]2019 Dec 12;9(1):18979. PMID: 31831831 -
J Food Sci
Sensing of L-Arginine by Gut-Expressed Calcium Sensing Receptor Stimulates Gut Satiety Hormones Cholecystokinin and Glucose-Dependent Insulinotropic Peptide Secretion in Pig Model. [Abstract]2018 Sep;83(9):2394-2401. PMID: 30088839 -
J Tradit Complement Med
Xinbao pill attenuated water retention by regulating the CaSR/AQP2 pathway in LAD-induced chronic heart failure rats. [Abstract]2024 Jul 2;15(5):495-508. PMID: 40979484 -
Photochem Photobiol
2022 Sep;98(5):1157-1166. PMID: 35288938 -
PeerJ
Cholesterol and steroid synthesis pathways may be involved in the inhibition of osteosarcoma cell viability by calcium-sensing receptor antagonism. [Abstract]2026 Jan 5:14:e20546. PMID: 41522513 -
Toxicon
Deoxynivalenol-induced anorexia is mediated by brain-gut peptides through CaSR-TRPM5 signaling axis. [Abstract]2026 Jan:269:108660. PMID: 41241198 -
FEBS Open Bio
Calcium-sensing receptor induces the apoptosis of chondrocytes in cooperation with phosphate transporter. [Abstract]2025 Oct 13. PMID: 41081312 -
FASEB Bioadv
2025 Sep 3;7(8):e70045. PMID: 40909871 -
Neurosci Lett
Inhibition of calcium-sensing receptor by its antagonist protects dopaminergic neurons from MPTP/MPP+-induced neurotoxicity via regulating mitochondrial function, autophagy, and apoptosis in vivo and in vitro. [Abstract]2025 Aug 9:865:138351. PMID: 40789434 -
Gen Comp Endocrinol
Phenylalanine and tryptophan stimulate gastrin and somatostatin secretion and H+-K+-ATPase activity in pigs through calcium-sensing receptor. [Abstract]2018 Oct 1:267:1-8. PMID: 29782837 -
J Vet Sci
Calcium-sensing receptor-mediated L-tryptophan-induced secretion of cholecystokinin and glucose-dependent insulinotropic peptide in swine duodenum. [Abstract]2018 Mar 31;19(2):179-187. PMID: 29284209
NPS-2143 purchased from MedChemExpress. Usage Cited in: J Vet Sci. 2018 Mar 31;19(2):179-187. [Abstract]
The protein levels of calcium-sensing receptor (CaSR) and its signal molecules regulated by CaSR antagonist NPS 2143. The protein images of CaSR, protein kinase C (PKC), and inositol trisphosphate receptor (IP3R) in the presence of 20 mM tryptophan and NPS 2143.
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Oxid Med Cell Longev
2021 Jan 12;2021:3010548. PMID: 33505580 -
Oxid Med Cell Longev
Expression and Role of the Calcium-Sensing Receptor in Rat Peripheral Blood Polymorphonuclear Neutrophils. [Abstract]2017:2017:3869561. PMID: 29081886
NPS-2143 purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2017:2017:3869561. [Abstract]
N-formyl-Met-Leu-Phe (fMLP; 10 nM) are used to stimulate the cells for 2 min, and the polymorphonuclear neutrophils (PMNs) without fMLP serve as the control. NPS-2143 (100 nM), Cinacalcet (100 nM), and PDTC (100 nM) are added and incubated. Protein expression results are representative of three experiments.
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (244.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
This clonal cell line, referred to as HEK 293 4.0-7 cells, are used in a high-throughput screening format to detect agonists and allosteric activators of the Ca2+ receptor. Changes in the concentration of cytoplasmic [Ca2+]i provide a quantitative and functional assessment of Ca2+ receptor activity in these cells and the results using this assay parallel those obtained using a homologous expression system of bovine parathyroid cells. On-line continuous measurements of fluorescence in fluo-3- or fura-2-loaded HEK 293 4.0-7 cells are obtained using a custom-built spectrofluorimeter or a fluorescence imaging plate reader instrument. NPS-2143 is incubated with cells for 1 minute before increasing the concentration of extracellular Ca2+ from 1.0 mM to 1.75 mM. NPS-2143 is tested individually at a concentration of 100 μg/mL (20 μM-80 μM) and those causing more than a 40% inhibition of the control response are considered to be biologically active. To determine the potencies (IC50) of NPS-2143 with biological activity, concentration-response curves are obtained and then, as an initial assessment of selectivity, the effects of NPS-2143 on [Ca2+]i evoked by other G protein-coupled receptors are examined at a concentration several times their IC50. Wild-type HEK 293 cells (and HEK 293 4.0-7 cells) express receptors for thrombin, bradykinin, and ATP, which couple to the mobilization of intracellular Ca2+. These responses can be studied to quickly assess any nonselective action of compounds on G protein-coupled receptors. Additional assays for selectivity include HEK 293 cells engineered to express receptors most homologous in sequence and topology to the Ca2+ receptor. These include native or chimeric receptors for various metabotropic glutamate and γ-aminobutyric acid type B receptors (GABABRs). Chimeric receptors are created using partial sequences of metabotropic glutamate receptors and Ca2+ receptors, engineered to couple to activation of phospholipase C and release of intracellular Ca2+ in HEK 293 cells. NPS-2143 lacking pan-activity are then subjected to structural modifications and their potencies and selectivities monitored using these HEK 293 4.0-7 cell assays in an iterative process.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats: On the day of study, the rats are infused intravenously (0.1 mL/kg·min) for 120 min with NPS-2143 (0.1 μmol/kg·min) or vehicle, a 20% aqueous solution of 2-hydroxypropyl-β-cyclodextrin. Blood samples (0.5 mL) are collected before and at various times after the start of the infusion for measurements of plasma levels of PTH and Ca2+. To prevent excessive blood volume loss during the course of the experiment, for each blood sample the erythrocyte pellet is resuspended in an equal volume of normal rat plasma and reinjected. Plasma levels of Ca2+ are measured immediately after collection using a model 634 ionized calcium analyzer. PTH levels are measured using the Immutopics rat PTH(1-34) immunoradiometric assay kit.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. 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. [Content Brief]
[2]. Rybczynska A, et al. Hypertensive effect of calcilytic NPS 2143 administration in rats. J Endocrinol. 2006 Oct;191(1):189-95. [Content Brief]
[3]. Ohsu T, et al. Involvement of the calcium-sensing receptor in human taste perception. J Biol Chem. 2010 Jan 8;285(2):1016-22 [Content Brief]
[4]. Nakajima S, et al. Calcium-sensing receptor mediates dietary peptide-induced CCK secretion in enteroendocrine STC-1 cells. Mol Nutr Food Res. 2012 May;56(5):753-60 [Content Brief]
[5]. Sun J, et al. Calcium-sensing receptor: a sensor and mediator of ischemic preconditioning in the heart. Am J Physiol Heart Circ Physiol. 2010 Nov;299(5):H1309-17. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4455 mL | 12.2273 mL | 24.4546 mL | 61.1366 mL |
| 5 mM | 0.4891 mL | 2.4455 mL | 4.8909 mL | 12.2273 mL | |
| 10 mM | 0.2445 mL | 1.2227 mL | 2.4455 mL | 6.1137 mL | |
| 15 mM | 0.1630 mL | 0.8152 mL | 1.6303 mL | 4.0758 mL | |
| 20 mM | 0.1223 mL | 0.6114 mL | 1.2227 mL | 3.0568 mL | |
| 25 mM | 0.0978 mL | 0.4891 mL | 0.9782 mL | 2.4455 mL | |
| 30 mM | 0.0815 mL | 0.4076 mL | 0.8152 mL | 2.0379 mL | |
| 40 mM | 0.0611 mL | 0.3057 mL | 0.6114 mL | 1.5284 mL | |
| 50 mM | 0.0489 mL | 0.2445 mL | 0.4891 mL | 1.2227 mL | |
| 60 mM | 0.0408 mL | 0.2038 mL | 0.4076 mL | 1.0189 mL | |
| 80 mM | 0.0306 mL | 0.1528 mL | 0.3057 mL | 0.7642 mL | |
| 100 mM | 0.0245 mL | 0.1223 mL | 0.2445 mL | 0.6114 mL |