2. GPCR/G Protein Neuronal Signaling Anti-infection
  3. Neurokinin Receptor Bacterial HIV Antibiotic
  4. Aprepitant

Aprepitant  (Synonyms: MK-0869; MK-869; L-754030)

Cat. No.: HY-10052 Purity: 99.91%
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Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.

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

Aprepitant Chemical Structure

Aprepitant Chemical Structure

CAS No. : 170729-80-3

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 78 In-stock
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10 mM * 1 mL in DMSO USD 78 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 79 In-stock
50 mg USD 106 In-stock
100 mg USD 131 In-stock
200 mg USD 158 In-stock
500 mg USD 198 In-stock
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Customer Review

Based on 10 publication(s) in Google Scholar

Aprepitant Related Antibodies

Top Publications Citing Use of Products

    Aprepitant purchased from MedChemExpress. Usage Cited in: Research Square Print. 2023 Mar 2.

    Aprepitant (10 mg/kg; i.p.; every 2 days for 21 days) remarkably reduces the volume and weight of mice intrahepatic cholangiocarcinoma (iCCA) xenograft tumors without affecting the body weight of nude mice.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.

    IC50 & Target

    Kd: 86 pM (Neurokinin 1 receptor)[1]
    In Vitro

    Aprepitant decreases the metabolic activity with an estimated IC50 value of 20 µM. Aprepitant induces cell-growth inhibition and G1 cell-cycle arrest. Aprepitant significantly induces apoptosis in Nalm-6 cells, and the apoptosis is mediated through caspase-3 activation. Aprepitant (20 µM) induces p53 accumulation and expression of pro-apoptotic p53 target genes[2]. Aprepitant (1, 5, 10 µM) inhibits HIV infection in MDM from both depressed and not depressed HIV negative individuals ex vivo in a dose-dependent manner. IC90 value of aprepitant is equivalent to 10 μM, and the IC50 value is about 5 μM[4].

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

    Aprepitant Related Antibodies
    In Vivo

    Aprepitant prevents the increase of NK-1R expression induced by in vivo NHP infection with B. burgdorferi. Aprepitant treatment prevents B. burgdorferi-induced increases in CCL2 protein levels in the CSF of NHPs. Aprepitant treatment prevents B. burgdorferi-induced increases in CCL2 and CXCL13 mRNA expression in the dorsal root ganglia of NHPs, prevents B. burgdorferi-induced increases in CCL2, CXCL13, IL-17A, and IL-6 mRNA expression in the spinal cord of NHPs. Aprepitant treatment attenuates B. burgdorferi infection-induced reductions in astrocyte activity/numbers[1]. Aprepitant (10 mg/kg, i.p.) significantly attenuates the CPP expression and locomotor activation produced by AMPH and cocaine in mice. Aprepitant does not induce significant CPP or conditioned place aversion or locomotor activation or suppression[3]. Aprepitant (125 mg/day, p.o.) results in 1 log reduction in plasma levels of viral RNA as compared to non-treated controls[4].

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

    534.43

    Formula

    C23H21F7N4O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1NC(CN2[C@H]([C@@H](O[C@@H](C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)C)OCC2)C4=CC=C(F)C=C4)=NN1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light

    *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (187.12 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8712 mL 9.3558 mL 18.7115 mL
    5 mM 0.3742 mL 1.8712 mL 3.7423 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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • 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 (4.68 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 (4.68 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).

    *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

    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: 99.91%

    COA (251 KB) LCMS (87 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    The inhibitory effect of aprepitant on metabolic activity of Nalm-6 cells is assessed by uptake of thiazolyl blue tetrazolium bromide (MTT) by viable cells. Cells are plated onto 96-well plates at a density of 5000 cells/well. After treatment with aprepitant at 5, 10, 15, 20 and 30 µM for 24, 36 and 48 h, the cells are further incubated with 100 μL of MTT (0.5 mg/mL) at 37°C for 3 h. Untreated cells are defined as the control group. Following solubilization of precipitated formazan with 100 μL of DMSO, the optical densitometry is measured with an ELISA reader at a wavelength of 578 nm.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Fifteen rhesus macaques are anesthetized and inoculated intrathecally with 1×108 live spirochetes into the cisterna magna, whereas five rhesus macaques are left uninfected and receive 1 mL of RPMI 1640 medium after removing an equivalent volume of CSF. The establishment of in vivo B. burgdorferi infection is confirmed by positive culture from at least necropsy tissue sample. The first set of animals are studied for 2 weeks and included two control animals (one of which is treated with aprepitant), two infected and untreated animals, and two infected animals that are treated with aprepitant. The second set of animals are studied for 4 weeks and included three control animals (one of which is treated with aprepitant), five infected and untreated animals, and four infected animals treated with aprepitant. Animals receive an average dose of aprepitant of 28 ± 6 mg/kg per day p.o. daily, and drug treatments are started 2 days before inoculation. These doses are consistent with standard veterinary regimens for the chosen drugs in NHP, and the 4-week duration of the study precludes the development of neural pathology that occurs at 8 weeks following B. burgdorferi infection.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8712 mL 9.3558 mL 18.7115 mL 46.7788 mL
    5 mM 0.3742 mL 1.8712 mL 3.7423 mL 9.3558 mL
    10 mM 0.1871 mL 0.9356 mL 1.8712 mL 4.6779 mL
    15 mM 0.1247 mL 0.6237 mL 1.2474 mL 3.1186 mL
    20 mM 0.0936 mL 0.4678 mL 0.9356 mL 2.3389 mL
    25 mM 0.0748 mL 0.3742 mL 0.7485 mL 1.8712 mL
    30 mM 0.0624 mL 0.3119 mL 0.6237 mL 1.5593 mL
    40 mM 0.0468 mL 0.2339 mL 0.4678 mL 1.1695 mL
    50 mM 0.0374 mL 0.1871 mL 0.3742 mL 0.9356 mL
    60 mM 0.0312 mL 0.1559 mL 0.3119 mL 0.7796 mL
    80 mM 0.0234 mL 0.1169 mL 0.2339 mL 0.5847 mL
    100 mM 0.0187 mL 0.0936 mL 0.1871 mL 0.4678 mL
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    Aprepitant 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:

    Aprepitant170729-80-3MK-0869 MK-869 L-754030MK0869MK 0869MK869MK 869MK-869L754030L 754030L-754030Neurokinin ReceptorBacterialHIVAntibioticNK receptorTachykinin receptorHuman immunodeficiency virusInhibitorinhibitorinhibit

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