2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. NKP608

NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.

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

NKP608 Chemical Structure

NKP608 Chemical Structure

CAS No. : 177707-12-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 355 In-stock
Solution
10 mM * 1 mL in DMSO USD 355 In-stock
Solid
5 mg USD 260 In-stock
10 mg USD 360 In-stock
50 mg USD 990 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

NKP608 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE NKP608

WB

    NKP608 purchased from MedChemExpress. Usage Cited in: Biol Res. 2018 May 30;51(1):14.  [Abstract]

    Effect of NKP608 on the expression of Bax, Bcl-2 and Caspase-3 protein are detected by western blot assay

    View All Neurokinin Receptor Isoform Specific Products:

    View All Isoforms
    NK1 NK2 NK3

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    NKP608 is a non-peptidic derivative of 4-aminopiperidine which acts as a selective, specific and potent antagonist at the neurokinin-1 (NK-1) receptor both in vitro(IC50=2.6 nM) and in vivo. IC50 value: 2.6 nM Target: NK-1 receptor In vitro, the binding of NKP608 to bovine retina was characterized by an IC50 of 2.6+/-0.4 nM, whereas the compound's affinity to other receptor binding sites, including NK-2 and NK-3, was much lower. Species differences in IC(50) values with NKP608 were less pronounced than with previously described NK-1 receptor antagonists, being 13+/-2 and 27+/-2 nM in gerbil midbrain and rat striatum, respectively. In vivo, using the hind foot thumping model in gerbils, NKP608 exhibited a potent NK-1 antagonistic activity following oral administration (ID(50)=0.23 mg/kg; 2 h pretreatment), supporting a central activity of NKP608. NKP608 may prove a useful anxiolytic compound.

    Molecular Weight

    619.98

    Formula

    C31H24ClF6N3O2
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(C1=CC=NC2=CC=CC=C12)N[C@@H]3C[C@@H](CC4=CC=C(Cl)C=C4)N(C(C5=CC(C(F)(F)F)=CC(C(F)(F)F)=C5)=O)CC3
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (161.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6130 mL 8.0648 mL 16.1296 mL
    5 mM 0.3226 mL 1.6130 mL 3.2259 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

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

      Solubility: ≥ 2.5 mg/mL (4.03 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.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (4.03 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.88%

    COA (256 KB) LCMS (93 KB)

    Handling Instructions (2659 KB)
    References

    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 1.6130 mL 8.0648 mL 16.1296 mL 40.3239 mL
    5 mM 0.3226 mL 1.6130 mL 3.2259 mL 8.0648 mL
    10 mM 0.1613 mL 0.8065 mL 1.6130 mL 4.0324 mL
    15 mM 0.1075 mL 0.5377 mL 1.0753 mL 2.6883 mL
    20 mM 0.0806 mL 0.4032 mL 0.8065 mL 2.0162 mL
    25 mM 0.0645 mL 0.3226 mL 0.6452 mL 1.6130 mL
    30 mM 0.0538 mL 0.2688 mL 0.5377 mL 1.3441 mL
    40 mM 0.0403 mL 0.2016 mL 0.4032 mL 1.0081 mL
    50 mM 0.0323 mL 0.1613 mL 0.3226 mL 0.8065 mL
    60 mM 0.0269 mL 0.1344 mL 0.2688 mL 0.6721 mL
    80 mM 0.0202 mL 0.1008 mL 0.2016 mL 0.5040 mL
    100 mM 0.0161 mL 0.0806 mL 0.1613 mL 0.4032 mL
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    NKP608 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.

    Keywords:

    NKP608177707-12-9NKP 608NKP-608Neurokinin ReceptorNK receptorTachykinin receptorInhibitorinhibitorinhibit

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