2. GPCR/G Protein Neuronal Signaling Stem Cell/Wnt Apoptosis Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK Cytoskeleton
  3. Neurokinin Receptor Wnt Bcl-2 Family β-catenin Cyclin G-associated Kinase (GAK) VEGFR Caspase Cadherin Apoptosis
  4. NKP608

NKP608 is a non-peptidic derivative of 4-aminopiperidine, a highly selective, orally active, neurokinin-1 (NK1) receptor antagonist with IC50 of 2.6 nM. NKP608 is active both in vitro and in vivo, showing extremely low affinity for NK2, NK3 receptors. NKP608 exerts its effects by blocking the NK₁ receptor, regulate cell proliferation and apoptosis, affect neurotransmitter functions and gastric mucosal repair mechanisms, and suppress the Wnt/β-catenin pathway in antitumor research. NKP608 is applicable to research related to various diseases, including cough, anxiety disorders, depression, gastric mucosal injury, and colorectal cancer.

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

CAS No. : 177707-12-9

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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
    NK1R NK2R NK3R

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    Wnt1 Wnt3 Wnt5 Wnt7 Wnt11

    View All Bcl-2 Family Isoform Specific Products:

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    Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

    View All Caspase Isoform Specific Products:

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    Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    NKP608 is a non-peptidic derivative of 4-aminopiperidine, a highly selective, orally active, neurokinin-1 (NK1) receptor antagonist with IC50 of 2.6 nM. NKP608 is active both in vitro and in vivo, showing extremely low affinity for NK2, NK3 receptors. NKP608 exerts its effects by blocking the NK₁ receptor, regulate cell proliferation and apoptosis, affect neurotransmitter functions and gastric mucosal repair mechanisms, and suppress the Wnt/β-catenin pathway in antitumor research. NKP608 is applicable to research related to various diseases, including cough, anxiety disorders, depression, gastric mucosal injury, and colorectal cancer[1][2][3][4][5][6][7].

    IC50 & Target[7]

    NK1R

    2.6 nM (IC50)

    Wnt3A

     

    Bcl-2

     

    Caspase 3

     

    Bax

     

    In Vitro

    NKP608 binds to human recombinant NK1 receptor with a pKi of 8.96, and shows lower affinity for human recombinant NK2 (pKi: 6.1) and NK3 (pKi: 6.25) receptors[1].
    NKP608 binds to NK1 receptor in bovine retina (IC50: 2.6 nM), gerbil midbrain (IC50: 13 nM) and rat striatum (IC50: 27 nM), and exhibits low affinity for NK2 receptor in bovine bladder (IC50: 2100 nM) and NK3 receptor in gerbil cortex (IC50: 1500 nM)[5].
    NKP608 (1 μM; 1 h) causes a 20-fold shift in the EC50 of substance P-induced inositol phosphate synthesis in rat cloned NK1 receptor-expressing CHO cells, and inhibits substance increase in acidification rate in rat NK1 receptor-expressing CHO cells[3].
    NKP608 (0.001-100 μM; 72 h) inhibits proliferation of human colorectal cancer HCT116 cells in a concentration-dependent manner[7].
    NKP608 (10 μM; 24 h) inhibits migration and invasion of human colorectal cancer HCT116 cells.NKP608 induces apoptosis of human colorectal cancer HCT116 cells, downregulates the expression of Bcl-2, and upregulates the expression of Bax and Active-Caspase-3. NKP608 reduces the expression of Wnt-3a, β-catenin, Cyclin D1 and VEGF, and induces the expression of E-Cadherin in human colorectal cancer HCT116 cells[7].

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

    NKP608 Related Antibodies

    Cell Viability Assay[7]

    Cell Line: HCT116 cells (human colorectal cancer)
    Concentration: 0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM, 100 μM
    Incubation Time: 72 h
    Result: Inhibits proliferation of HCT116 cells in a concentration-dependent manner.

    Cell Proliferation Assay[7]

    Cell Line: HCT116 cells (human colorectal cancer)
    Concentration: 10 μM
    Incubation Time: 24 h, 48 h, 72 h
    Result: Significantly inhibits migration of HCT116 cells.

    Cell Invasion Assay[7]

    Cell Line: HCT116 cells (human colorectal cancer)
    Concentration: 10 μM
    Incubation Time: 24 h
    Result: Significantly inhibits invasion of HCT116 cells.

    Apoptosis Analysis[7]

    Cell Line: HCT116 cells (human colorectal cancer)
    Concentration: 10 μM
    Incubation Time: 24 h
    Result: Induces apoptosis of HCT116 cells.

    Western Blot Analysis[7]

    Cell Line: HCT116 cells (human colorectal cancer)
    Concentration: 10 μM
    Incubation Time: 24 h
    Result: Downregulates expressions of Bcl-2, Wnt-3a, β-catenin, Cyclin D1 and VEGF; upregulates expressions of Bax, Active-Caspase-3 and E-Cadherin.
    In Vivo

    NKP608 (0.03, 0.3, 1 mg/kg; p.o.; once; 2 h prior to challenge) significantly reduces citric acid-induced cough in Dunkin Hartley guinea pigs[1].
    NKP608 (0.003, 0.03, 0.3 mg/kg; p.o.; once; 90 min prior to test) exerts anxiolytic-like effects in male spontaneously hypertensive rats (SHR) in the open field test and partial anxiolytic-like effects in male Lewis rats in the elevated plus-maze (EPM) test[2].
    NKP608 (0.2 mg/kg; i.v.; once; immediately prior to agonist challenge) potently inhibits GR73632 (HY-P1192)-induced foot drumming in Mongolian gerbils[3].
    NKP608 (0.01, 0.1, 0.3 mg/kg; p.o.; once; 2 h prior to test) increases social investigation time in Mongolian gerbils, showing robust anxiolytic effects[4].
    NKP608 (0.03-3 mg/kg; p.o.; once; 2, 5 or 24 h prior to agonist administration) dose-dependently inhibits SPOMe-induced hind foot thumping in Mongolian gerbils with ID50 values of 0.23 mg/kg (2 h), 0.15 mg/kg (5 h) and 0.38 mg/kg (24 h), respectively[5].
    NKP608 (0.01-1 mg/kg; p.o.; once; 90 min prior to test) specifically increases active social interaction time in Sprague-Dawley rats in a highly illuminated unfamiliar arena[5].
    NKP608 (0.03-3 mg/kg; p.o.; once; 90 min prior to test) increases social exploration time of intruder rats towards resident rats in Sprague-Dawley rats[5].
    NKP608 (1 mg/kg; i.g.; once daily; for 8 consecutive days) delays gastric cryoulcer healing and decreases the number of Ki-67-positive epithelial cells in the ulcer margin in both wild-type and COX-2-/- mice[6].

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

    Animal Model: Dunkin Hartley guinea pigs (250-500 g; no gender specified) were exposed to nebulized citric acid (0.6 M) for 10 min to induce cough and airway obstruction[1].
    Dosage: NKP608: 0.03, 0.3, 1 mg/kg; single drug administration
    Administration: Oral (p.o.) administration; once; 2 h prior to citric acid challenge
    Result: Significantly reduces the number of citric acid-induced coughs by 77% (0.03 mg/kg), 74% (0.3 mg/kg) and 79% (1 mg/kg), respectively; does not significantly reduce citric acid-induced increase in enhanced pause (Penh).
    Animal Model: Male spontaneously hypertensive rats (SHR) and male Lewis rats (9 weeks old; body weight: SHR males 232 g, LEW males 234 g) were subjected to elevated plus-maze (EPM) and open field (OF) tests to evaluate anxiety-related behaviors[2].
    Dosage: 0.003, 0.03, 0.3 mg/kg
    Administration: Oral (p.o.) administration; once; 90 min prior to tests
    Result: Exerts anxiolytic-like effects in male SHR rats in the OF test.
    Shows partial anxiolytic-like effects in male Lewis rats in the EPM test .
    Has no significant anxiolytic effects in female SHR or Lewis rats in either test.
    Animal Model: Mongolian gerbils (40-60 g; no gender specified) were intracerebroventricularly (i.c.v.) injected with GR73632 (3 pmol/5 μL) to induce foot drumming behavior[3].
    Dosage: 0.2 mg/kg
    Administration: Intravenous (i.v.) injection; once; immediately prior to GR73632 administration
    Result: Potently inhibits GR73632-induced foot drumming in Mongolian gerbils.
    Animal Model: Mongolian gerbils (70-85 g; male) were subjected to the social investigation test to evaluate anxiety-related behaviors[4].
    Dosage: 0.01, 0.1, 0.3 mg/kg
    Administration: Oral (p.o.) administration; once; 2 h prior to test
    Result: Increases the time of social investigation towards an untreated, unfamiliar partner.
    Animal Model: Mongolian gerbils (70-80 g; male) were intracerebroventricularly (i.c.v.) injected with SPOMe (1 μg/5 μL) to induce hind foot thumping behavior[5].
    Dosage: 0.1, 0.3 mg/kg
    Administration: Oral (p.o.) administration; once daily; for 7 consecutive days
    Result: Attenuates SPOMe-induced hind foot thumping when tested 2 h or 24 h after the last administration.
    Animal Model: Sprague-Dawley rats (180-200 g; male) were subjected to the social interaction test in a highly illuminated unfamiliar arena (65×65×45 cm)[5].
    Dosage: 0.001 mg/kg, 0.01 mg/kg, 0.1 mg/kg, 1 mg/kg
    Administration: Oral (p.o.) administration; once; 90 min prior to test
    Result: Specifically increases active social interaction time between unfamiliar rats and does not affect general activity parameters.
    Animal Model: Wild-type and COX-2-/- mice (20-24 g; female; 7-8 weeks old) were subjected to laparotomy to induce gastric cryoulcers via serosal application of a CO2-cooled cryoprobe (15 s)[6].
    Dosage: 1 mg/kg
    Administration: Intragastric (i.g.) administration; once daily; for 8 consecutive days
    Result: Delays gastric cryoulcer healing in both wild-type and COX-2⁻/⁻ mice and decreases the number of Ki-67-positive epithel.
    Animal Model: Sprague-Dawley rats (residents: 350-400 g, male; intruders: 100-120 g, male, Lister Hooded strain) were subjected to the social exploration test[5].
    Dosage: 0.03 mg/kg, 0.3 mg/kg, 3 mg/kg
    Administration: Oral (p.o.) administration; once; 90 min prior to test (administered to intruder rats only)
    Result: Increases the time of active social exploration of intruder rats towards resident rats.
    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.

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    Concentration (start)

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    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
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    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%

    SDS (251 KB)

    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 ReceptorWntBcl-2 Familyβ-cateninCyclin G-associated Kinase (GAK)VEGFRCaspaseCadherinApoptosisNK receptorTachykinin receptorBeta cateninAuxilin 2Vascular endothelial growth factor receptorselective NK? receptor antagonistorally activeblood-brain barrier-penetrantcompetitive binding propertyinhibits tachykinin-mediated signaling pathwaysuppresses Wnt/β-catenin pathwayU-373MG cellsAR42J cellsCHO cellsHCT116 cellsCCD841 cellsDunkin Hartley guinea pigsLewis ratsspontaneously hypertensive rats (SHR)Mongolian gerbilsSprague-Dawley ratsCOX-2?/? micewild-type micecoughanxiety disordersdepressiongastric mucosal injurycolorectal cancerInhibitorinhibitorinhibit

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