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Technical Data
| Formula | C24H25ClN2O2 |
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| Molecular Weight | 408.92 | CAS No. | 284035-33-2 | |
| Solubility (25°C)* | In vitro | DMSO | 82 mg/mL (200.52 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | NPS-2143 (SB262470) is a novel potent and selective antagonist of Ca(2+) receptor with IC50 of 43 nM. | ||
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| In vitro | NPS 2143 blocks increases in cytoplasmic Ca2+ concentrations with IC50 of 43 nM elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor. [1] NPS 2143 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 (data not shown) and γ-Glu-Val-Gly. [3] A recent study shows that NPS 2143 treatment suppresses low molecular weight fractions of azuki hydrolysate-induced cholecystokinin (CCK) secretion in CaSR-transfected HEK 293 cells. [4] | ||
| In vivo | In rats, NPS 2143 results in a rapid 4- to 5-fold increase in plasma PTH levels and also a transient increase in plasma Ca2+ levels. [1] In normotensive rats, NPS 2143 administration (1 mg/kg) by i.v. markedly increases mean arterial blood pressure (MAP) in the presence of parathyroid glands. [2] |
Protocol (from reference)
| Animal Study:[1] |
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References
Customer Product Validation
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Data from [Data independently produced by J Biol Chem, 2014, 289(42), 28835-45]
Selleck's NPS-2143 has been cited by 20 publications
| The role of calcium-sensing receptor in ginsenoside Rg1 promoting reendothelialization to inhibit intimal hyperplasia after balloon injury [ Biomed Pharmacother, 2023, 163:114843] | PubMed: 37201261 |
| Revitalizing Skin Repair: Unveiling the Healing Power of Livisin, a Natural Peptide Calcium Mimetic [ Toxins (Basel), 2023, 16(1)21] | PubMed: 38251238 |
| The role of calcium-sensitive receptor in ovalbumin-induced airway inflammation and hyperresponsiveness in juvenile mice with asthma [ Kaohsiung J Med Sci, 2022, 10.1002/kjm2.12601] | PubMed: 36169192 |
| Oat β-glucan ameliorates epidermal barrier disruption by upregulating the expression of CaSR through dectin-1-mediated ERK and p38 signaling pathways [ Int J Biol Macromol, 2021, 185:876-889] | PubMed: 34237364 |
| Tryptophan Ameliorates Barrier Integrity and Alleviates the Inflammatory Response to Enterotoxigenic Escherichia coli K88 Through the CaSR/Rac1/PLC-γ1 Signaling Pathway in Porcine Intestinal Epithelial Cells [ Front Immunol, 2021, 12:748497] | PubMed: 34745120 |
| Tryptophan improves porcine intestinal epithelial cell restitution through the CaSR/Rac1/PLC-γ1 signaling pathway [ Food Funct, 2021, 10.1039/d1fo01075a] | PubMed: 34374393 |
| Sustained calcium ion release from bioceramics promotes CaSR-mediated M2 macrophage polarization for osteoinduction [ J Leukoc Biol, 2021, 110(3):485-496] | PubMed: 34184323 |
| Calcium-sensing receptor protects intestinal integrity and alleviates the inflammatory response via the Rac1/PLCγ1 signaling pathway [ Anim Biotechnol, 2021, 1-14] | PubMed: 34762003 |
| Effect of calcium-sensing receptor on the migration and proliferation of porcine intestinal epithelial cells [ Anim Biotechnol, 2021, 1-10] | PubMed: 34459707 |
| Ginsenoside Rg1 attenuates mechanical stress-induced cardiac injury via calcium sensing receptor-related pathway [ J Ginseng Res, 2021, 45(6):683-694] | PubMed: 34764723 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.