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  3. CaSR
  4. NPS-2143 hydrochloride

NPS-2143 hydrochloride  (Synonyms: SB-262470A hydrochloride)

Cat. No.: HY-10171 Purity: 99.80%
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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.

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 114 In-stock
Solution
10 mM * 1 mL in DMSO USD 114 In-stock
Solid
1 mg USD 49 In-stock
5 mg USD 104 In-stock
10 mg USD 160 In-stock
50 mg USD 431 In-stock
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Customer Review

Based on 18 publication(s) in Google Scholar

Other Forms of NPS-2143 hydrochloride:

NPS-2143 hydrochloride Related Antibodies

Top Publications Citing Use of Products

    NPS-2143 hydrochloride 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.

    NPS-2143 hydrochloride 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.

    NPS-2143 hydrochloride 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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    • Customer Review

    Description

    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].

    In Vitro

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    NPS-2143 hydrochloride Related Antibodies
    In Vivo

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    445.38

    Appearance

    Solid

    Formula

    C24H26Cl2N2O2
    CAS No.
    SMILES

    N#CC1=C(OC[C@@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

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (224.53 mM)

    H2O : 1.85 mg/mL (4.15 mM; ultrasonic and warming and heat to 60°C)

    *"≥" 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 available by MedChemExpress (MCE).
    Purity & Documentation
    References
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    NPS-2143 hydrochloride Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    NPS-2143324523-20-8SB-262470ANPS2143NPS 2143CaSRCalcium-sensing receptorInhibitorinhibitorinhibit

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