2. Immunology/Inflammation
  3. Toll-like Receptor (TLR)
  4. Motolimod

Motolimod (VTX-2337;VTX-378) is a selective Toll-like receptor 8 (TLR8) agonist, with an EC50 of approximately 100 nM.

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No. CAS : 926927-61-9

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Revisión del cliente

Based on 13 publication(s) in Google Scholar

Other Forms of Motolimod:

Motolimod Related Antibodies

Top Publications Citing Use of Products

    Motolimod purchased from MedChemExpress. Usage Cited in: ACS Nano. 2023 Aug 8;17(15):14424-14441.  [Abstract]

    Repolarization of tumor-associated macrophages. qRT−PCR analysis of the expression of Arg1, CD206, iNOS, and TNF-α in 4T1-TAMs and Hepa1-6-TAMs treated with the supernatant of tumor cells, M (Motolimod; 0.1 μg; for 24 h), NPs (M), NPs (M+C), NPs (M+siPD-L1), and NPs (M+C+siPD-L1). The data are shown as the mean ± SEM (n = 3).

    Motolimod purchased from MedChemExpress. Usage Cited in: Rheumatology (Oxford). 2024 May 3;63(6):1710-1719.  [Abstract]

    The effects of VTX-2337 (Motolimod; 10 μM) on expression of smad2/3 and P-smad2/3 induced by TGF-β (10 ng/ml) in healthy skin fibroblasts. Data are represented as mean (s.d.). *P < 0.05. **P < 0.01, ***P < 0.001, ****P < 0.0001

    Motolimod purchased from MedChemExpress. Usage Cited in: Rheumatology (Oxford). 2024 May 3;63(6):1710-1719.  [Abstract]

    TLR8 gene silencing inhibited the upregulation of IL-6 (protein and mRNA), TNF-α (protein and mRNA) induced by VTX-2337 (Motolimod; 10 μM).

    Motolimod purchased from MedChemExpress. Usage Cited in: Rheumatology (Oxford). 2024 May 3;63(6):1710-1719.  [Abstract]

    Cu-cpt-8m (HY-112050; 60 μM) inhibited the upregulation of IL-6, IL-1β, TNF-α, COLI and COLIII induced by VTX-2337 (Motolimod; HY-13773; 10 μM).

    Motolimod purchased from MedChemExpress. Usage Cited in: Cell Rep. 2021 Feb 2;34(5):108724.  [Abstract]

    Primary intestinal NFs were exposed to TLR agonists and IL-1 for 12 h, and OPN mRNA was measured using qPCR analysis. The results were normalized to β-actin. ∗p < 0.05. TLR agonists were used at the following concentrations: TLR1/2 agonist (Pam3CSK4), 100 ng/mL; TLR4 agonist (LPS), 1 μg/mL; TLR7 agonist (Imiquimod; HY-B0180), 100 ng/mL; TLR8 agonist (Motolimod; HY-13773), 250 ng/mL; and IL-1, 5 ng/ml.

    Motolimod purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2017 Feb 17;292(7):2805-2814.  [Abstract]

    IL-1β ELISAs of supernatants from THP1 that are pre-incubated with medium or the indicated TLR8 agonists CL075 (5 μg/mL) or VTX-2337 (10 μM) for 16 h and after 8 h incubation in TLR8 agonist-free medium stimulated with 0.5 mg/mL ABC or medium for additional 16 h, respectively.

    Ver todos los productos específicos de isoformas Toll-like Receptor (TLR):

    Ver todas las isoformas
    TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

    • Actividad biológica

    • Protocolo

    • Pureza y Documentación

    • Referencias

    • Revisión del cliente

    Descripciòn

    Motolimod (VTX-2337;VTX-378) is a selective Toll-like receptor 8 (TLR8) agonist, with an EC50 of approximately 100 nM.

    IC50 & Target

    TLR8

     

    In Vitro

    Among the TLRs tested (TLR2, 3, 4, 5, 7, 8, and 9), Motolimod (VTX-2337) selectively activates TLR8. Motolimod stimulates the production of both TNFα (EC50=140±30 nM based on 10 donors) and IL-12 (EC50=120±30 nM based on 10 donors) in PBMCs. The EC50 value for MIP-1β induction is 60 nM for Motolimod[1].

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

    Motolimod Related Antibodies
    In Vivo

    Monkeys receive a subcutaneous injection of Motolimod (1 or 10 mg/kg), and plasma is collected predose, 6, 12, 24, and 96 h post-injection. For the 10 mg/kg dose, mean plasma levels of IL-1β increase from baseline levels of 0.5 pg/mL, up to 9.12±2.7 ng/mL (p<0.05, t-test) at 6 h post-administration of Motolimod (10 mg/kg). Circulating levels of IL-18 also increase from a baseline of ~ 1 pg/mL to 68.7±4.4 pg/mL (p<0.05, t-test) at 6 h in response to the Motolimod (VTX-2337) treatment (10 mg/kg). Levels of IL-6 are monitored, as this mediator is induced in response to TLR8 activation, but the release is independent of NLRP3 inflammasome activation. In addition, plasma levels of IFNγ are assessed as a measure of NK cell activation in response to Motolimod treatment[2].

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

    458.60

    Fòrmula

    C28H34N4O2
    No. CAS
    Appearance

    Solid

    Color

    Light yellow to brown

    SMILES

    O=C(C1=CC2=CC=C(C3=CC=C(C(N4CCCC4)=O)C=C3)C=C2N=C(N)C1)N(CCC)CCC
    Envío

    Room temperature in continental US; may vary elsewhere.
    Almacenamiento
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvente y solubilidad
    In Vitro: 

    DMSO : 50 mg/mL (109.03 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 2.1805 mL 10.9027 mL 21.8055 mL
    5 mM 0.4361 mL 2.1805 mL 4.3611 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.

    • Calculadora de molaridad

    • Calculadora de dilución

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    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 (5.45 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.45 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    +
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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.
    Pureza y Documentación

    Purity: 98.10%

    SDS (393 KB)

    COA (250 KB) HNMR (140 KB) RP-HPLC (248 KB) MS (68 KB)

    Instrucciones de manejo (2659 KB)
    Referencias
    Ensayo de quinasas
    [1]

    Human embryonic kidney cells (HEK293) expressing TLR2, 3, 4, 5, 7, 8, or 9 are cultured in Dulbecco's Modified Eagle's Media containing 4.5 g/L L-glucose and 10% FBS. The activity of specific TLR agonists is assessed using the secretory embryonic alkaline phosphatase (SEAP) reporter gene that is linked to NF-κB activation in response to TLR stimulation. Measurement of SEAP activity using the Quanti-blue substrate after TLR agonist treatment is carried out similarly[1].

    MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
    Ensayo celular
    [1]

    PBMCs or purified NK cells are prepared, and the purity of NK cells is approximately 99%. NK cell-mediated cytotoxicity is assessed by Calcein AM release from labeled target cells. In brief, PBMCs or purified NK cells are cultured for 48 hours in RPMI medium in the presence of Motolimod (167 or 500 nM) before incubation with target cells[1].

    MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
    Administraciòn de animales
    [2]

    Monkeys[2]
    The male monkeys (2.9-4.9 kg) are housed individually (cage dimensions of 0.76 m wide×0.74 m deep×0.81 m in height), but commingled periodically as part of the environmental enrichment program. The animals are also given fruit, vegetable, or additional supplements as a form of environmental enrichment, as well as given various cage enrichment devices. Animals are given Certified Primate Diet, two times daily and water ad libitum. Motolimod is administered as a bolus subcutaneous (SC) injection in the intrascapular area at doses of 1 and 10 mg/kg. Blood samples are collected at baseline (pre-dose), and 6, 12, 24, and 96 h post injection to monitor levels of IL-1β and IL-18 in the plasma using the human MAP v.1.6 inflammation panel.

    MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
    Referencias

    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 2.1805 mL 10.9027 mL 21.8055 mL 54.5137 mL
    5 mM 0.4361 mL 2.1805 mL 4.3611 mL 10.9027 mL
    10 mM 0.2181 mL 1.0903 mL 2.1805 mL 5.4514 mL
    15 mM 0.1454 mL 0.7268 mL 1.4537 mL 3.6342 mL
    20 mM 0.1090 mL 0.5451 mL 1.0903 mL 2.7257 mL
    25 mM 0.0872 mL 0.4361 mL 0.8722 mL 2.1805 mL
    30 mM 0.0727 mL 0.3634 mL 0.7268 mL 1.8171 mL
    40 mM 0.0545 mL 0.2726 mL 0.5451 mL 1.3628 mL
    50 mM 0.0436 mL 0.2181 mL 0.4361 mL 1.0903 mL
    60 mM 0.0363 mL 0.1817 mL 0.3634 mL 0.9086 mL
    80 mM 0.0273 mL 0.1363 mL 0.2726 mL 0.6814 mL
    100 mM 0.0218 mL 0.1090 mL 0.2181 mL 0.5451 mL
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    Motolimod 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:

    Motolimod926927-61-9VTX-2337 VTX-378VTX2337VTX 2337VTX378VTX 378VTX-378Toll-like Receptor (TLR)Inhibitorinhibitorinhibit

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