1. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  2. nAChR 5-HT Receptor
  3. PNU-282987

PNU-282987 

Cat. No.: HY-12560A Purity: 99.52%
COA Handling Instructions

PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 can be used for the research of central and peripheral nervous systems.

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

PNU-282987 Chemical Structure

PNU-282987 Chemical Structure

CAS No. : 123464-89-1

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 87 In-stock
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10 mM * 1 mL in DMSO USD 87 In-stock
Solid
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10 mg USD 79 In-stock
50 mg USD 288 In-stock
100 mg USD 528 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of PNU-282987:

Top Publications Citing Use of Products

    PNU-282987 purchased from MedChemExpress. Usage Cited in: Inflamm Res. 2023 Mar 13.  [Abstract]

    PNU-282987 (3 mg/kg; i.p.; single daily for consecutively 28 days) signifcantly decreases the expression levels of collagen I, collagen III, and α-SMA in myocardial infarction (MI) rats model, while Methyllycaconitine citrate (MLA; 3 mg/kg; i.p.; single daily for consecutively 28 days) increases these proteins levels.
    • Biological Activity

    • Purity & Documentation

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    • Customer Review

    Description

    PNU-282987 is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 can be used for the research of central and peripheral nervous systems[1].

    IC50 & Target

    IC50: 4541nM (5-HT3); EC50: 154 nM (α7 nAChR); Ki: 27 nM (R7 MLA)[1]

    In Vitro

    PNU-282987 (Compound C7) displaces the R7 selective antagonist methyllycaconitine (MLA) from rat brain homogenates with a Ki of 27 nM[1].
    PNU-282987 has α7 nAChR agonist activity with an EC50 of 154 nM[1].
    PNU-282987 also has inhibition for the 5-HT3 receptor with an IC50 value of 4541nM[1].

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

    In Vivo

    PNU-282987 (Compound C7) (i.v.; 1, 3 mg/kg) leads to a reversal of the gating deficit[1].
    PNU-282987 (30 μM) evokes currents in rat hippocampal neurons in a concentration-dependent and MLA blockable manner[1].

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

    Animal Model: Rats[1]
    Dosage: 1, 3 mg/kg
    Administration: i.v.
    Result: Significantly reversed amphetamine-induced gating deficit.
    Molecular Weight

    301.21

    Formula

    C14H18Cl2N2O

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=CC=C(C=C1)Cl)N[C@H]2CN3CCC2CC3.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    H2O : 50 mg/mL (166.00 mM; Need ultrasonic)

    DMSO : 10 mg/mL (33.20 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.3199 mL 16.5997 mL 33.1994 mL
    5 mM 0.6640 mL 3.3199 mL 6.6399 mL
    10 mM 0.3320 mL 1.6600 mL 3.3199 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  PBS

      Solubility: 50 mg/mL (166.00 mM); Clear solution; Need ultrasonic

    • 2.

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

      Solubility: 1 mg/mL (3.32 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 1 mg/mL (3.32 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.70%

    References
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    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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    Product Name:
    PNU-282987
    Cat. No.:
    HY-12560A
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