1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)

Motolimod (Synonyms: VTX-2337; VTX-378)

Cat. No.: HY-13773 Purity: 98.83%
Handling Instructions

Motolimod is a selective Toll-like receptor (TLR) 8 agonist, with EC50 of about 100 nM.

For research use only. We do not sell to patients.
Motolimod Chemical Structure

Motolimod Chemical Structure

CAS No. : 926927-61-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 224 In-stock
5 mg USD 204 In-stock
10 mg USD 324 In-stock
25 mg USD 588 In-stock
50 mg USD 840 In-stock
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    Motolimod purchased from MCE. Usage Cited in: J Biol Chem. 2017 Feb 17;292(7):2805-2814.

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Motolimod is a selective Toll-like receptor (TLR) 8 agonist, with EC50 of about 100 nM.

    IC50 & Target

    EC50: 100 nM (TLR8)[1]

    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].

    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].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.2181 mL 1.0903 mL 2.1805 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [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 has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    Motolimod (VTX-2337) is dissolved in DMSO and stored, and then diluted with appropriate media before use[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 has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Motolimod (VTX-2337) is dissolved in DMSO and diluted with PBS before use (Monkeys)[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 has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    458.6

    Formula

    C₂₈H₃₄N₄O₂

    CAS No.

    926927-61-9

    SMILES

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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 98.83%

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    Inquiry Information

    Product Name:
    Motolimod
    Cat. No.:
    HY-13773
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