1. GPCR/G Protein
  2. CaSR
  3. NPS-2143 hydrochloride

NPS-2143 hydrochloride 

Cat. No.: HY-10171 Purity: 99.96%
Handling Instructions

NPS-2143 hydrochloride is a selective potent calcium ion-sensing receptor antagonist with IC50 of 43 and 41 nM for cytoplasmic Ca2+ concentrations and parathyroid hormone secretion, respectively.

For research use only. We do not sell to patients.

NPS-2143 hydrochloride Chemical Structure

NPS-2143 hydrochloride Chemical Structure

CAS No. : 324523-20-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 114 In-stock
Estimated Time of Arrival: December 31
5 mg USD 104 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
50 mg USD 431 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of NPS-2143 hydrochloride:

Top Publications Citing Use of Products

    NPS-2143 hydrochloride purchased from MCE. Usage Cited in: Am J Physiol Heart Circ Physiol. 2010 Nov;299(5):H1309-17.

    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.

    NPS-2143 hydrochloride purchased from MCE. Usage Cited in: J Vet Sci. 2018 Mar 31;19(2):179-187.

    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.

    NPS-2143 hydrochloride purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:3869561.

    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.
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    Description

    NPS-2143 hydrochloride is a selective potent calcium ion-sensing receptor antagonist with IC50 of 43 and 41 nM for cytoplasmic Ca2+ concentrations and parathyroid hormone secretion, respectively. IC50 value: 43 nM(for Ca2+ receptor) [1] Target: CaSR in vitro: NPS-2143, even when tested at much higher concentrations (3 microM), did not affect the activity of a number of other G protein-coupled receptors, including those most structurally homologous to the Ca2+ receptor. NPS-2143 stimulated parathyroid hormone (PTH) secretion from bovine parathyroid cells (EC50 of 41 nM) over a range of extracellular Ca2+ concentrations and reversed the effects of the calcimimetic compound NPS R-467 on [Ca2+]i and on secretion of PTH [1]. The first reported calcilytic compound was NPS-2143, an orally active molecule which elicits rapid, 3- to 4-fold increases in circulating levels of PTH [2]. in vivo: When infused intravenously in normal rats, NPS-2143 caused 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].

    Molecular Weight

    445.38

    Formula

    C₂₄H₂₆Cl₂N₂O₂

    CAS No.

    324523-20-8

    SMILES

    N#CC1=C(OC[[email protected]@H](CNC(C)(C)CC2=CC=C3C=CC=CC3=C2)O)C=CC=C1Cl.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (224.53 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
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    NPS-2143 hydrochloride
    Cat. No.:
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