Motolimod
Based on 14 publication(s) in Google Scholar
Motolimod (VTX-2337;VTX-378) is a selective Toll-like receptor 8 (TLR8) agonist, with an EC50 of approximately 100 nM.
For research use only. We do not sell to patients.
- Purity: 98.10%
- CAS No.: 926927-61-9
- Formula: C28H34N4O2
- Molecular Weight:458.60
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Motolimod
More- Nat Biomed Eng. 2018 Aug;2(8):578-588. [Abstract]
- ACS Nano. 2023 Aug 8;17(15):14424-14441. [Abstract]
- Hepatology. 2025 Nov 7. [Abstract]
- J Extracell Vesicles. 2025 May;14(5):e70083. [Abstract]
- J Control Release. 2021 Feb 10;330:1080-1094. [Abstract]
- J Exp Med. 2019 Feb 4;216(2):384-406. [Abstract]
- Cell Rep. 2021 Feb 2;34(5):108724. [Abstract]
- J Invest Dermatol. 2017 Feb;137(2):367-376. [Abstract]
- Cancer Immunol Immunother. 2026 Feb 12;75(3):77. [Abstract]
- Rheumatology (Oxford). 2024 May 3;63(6):1710-1719. [Abstract]
- J Biol Chem. 2017 Feb 17;292(7):2805-2814. [Abstract]
- bioRxiv. 2026 Apr 29.
- Theriogenology Wild. 2025.
- bioRxiv. 2024 July 25.
Customer Validation & Images
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RT-PCR
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WB
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RT-PCR
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RT-PCR
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RT-PCR
Biological Activity
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TLR8 |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 926927-61-9
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Appearance Solid
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Molecular Weight 458.60
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Formula C28H34N4O2
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Color Light yellow to brown
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SMILES
O=C(C1=CC2=CC=C(C3=CC=C(C(N4CCCC4)=O)C=C3)C=C2N=C(N)C1)N(CCC)CCC
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Synonyms
VTX-2337; VTX-378
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (14)
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Journal Impact Factor
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Most Recent
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Nat Biomed Eng
TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]2018 Aug;2(8):578-588. PMID: 31015631 -
ACS Nano
Multifunctional Redox-Responsive Nanoplatform with Dual Activation of Macrophages and T Cells for Antitumor Immunotherapy. [Abstract]2023 Aug 8;17(15):14424-14441. PMID: 37498878
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).
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Hepatology
GPC3-based circular RNA vaccine suppresses hepatocellular carcinoma progression by activating adaptive immune responses. [Abstract]2025 Nov 7. PMID: 41201153 -
J Extracell Vesicles
Cancer-Specific RNA Modifications in Tumour-Derived Extracellular Vesicles Promote Tumour Growth. [Abstract]2025 May;14(5):e70083. PMID: 40326665 -
J Control Release
Development of thermosensitive resiquimod-loaded liposomes for enhanced cancer immunotherapy. [Abstract]2021 Feb 10;330:1080-1094. PMID: 33189786 -
J Exp Med
Immune regulation by glucocorticoids can be linked to cell type-dependent transcriptional responses. [Abstract]2019 Feb 4;216(2):384-406. PMID: 30674564 -
Cell Rep
MyD88 in myofibroblasts enhances colitis-associated tumorigenesis via promoting macrophage M2 polarization. [Abstract]2021 Feb 2;34(5):108724. PMID: 33535045
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.
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J Invest Dermatol
Allergy-Inducing Chromium Compounds Trigger Potent Innate Immune Stimulation Via ROS-Dependent Inflammasome Activation. [Abstract]2017 Feb;137(2):367-376. PMID: 27751866 -
Cancer Immunol Immunother
TLR8 agonists remodel the tumor immune microenvironment through PF4-dependent T cell recruitment and ancillary mechanisms. [Abstract]2026 Feb 12;75(3):77. PMID: 41677949 -
Rheumatology (Oxford)
TLR8 aggravates skin inflammation and fibrosis by activating skin fibroblasts in systemic sclerosis. [Abstract]2024 May 3;63(6):1710-1719. PMID: 37665747
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).
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J Biol Chem
Potent NLRP3 Inflammasome Activation by the HIV Reverse Transcriptase Inhibitor Abacavir. [Abstract]2017 Feb 17;292(7):2805-2814. PMID: 28057759
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.
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Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Lu H, et al. VTX-2337 is a novel TLR8 agonist that activates NK cells and augments ADCC. Clin Cancer Res. 2012 Jan 15;18(2):499-509. [Content Brief]
[2]. Dietsch GN, et al. Coordinated Activation of Toll-Like Receptor8 (TLR8) and NLRP3 by the TLR8 Agonist, VTX-2337, Ignites Tumoricidal Natural Killer Cell Activity. PLoS One. 2016 Feb 29;11(2):e0148764. [Content Brief]
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 |
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| 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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