Referencia número: HY-13773

Motolimod

(Synonyms: VTX-2337; VTX-378)

14 Cited Publications

Revisión del cliente

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.

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Pureza: 98.10%
No. CAS: 926927-61-9
Fòrmula: C₂₈H₃₄N₄O₂
Peso molecular:458.60

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Motolimod Chemical Structure

No. CAS: 926927-61-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (14)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

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

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

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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 926927-61-9
Appearance Solid
Peso molecular 458.60
Fòrmula C₂₈H₃₄N₄O₂
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
Synonyms

VTX-2337; VTX-378
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

Publications (14)

All RT-PCRWB

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Journal Impact Factor

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
J Extracell Vesicles

Cancer-Specific RNA Modifications in Tumour-Derived Extracellular Vesicles Promote Tumour Growth. [Abstract]

2025 May;14(5):e70083. PMID: 40326665
Hepatology

GPC3-based circular RNA vaccine suppresses hepatocellular carcinoma progression by activating adaptive immune responses. [Abstract]

2025 Nov 7. PMID: 41201153
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).
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.
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).
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.
Theriogenology Wild

2025.
bioRxiv

2026 Apr 29.
bioRxiv

2024 July 25.

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.45 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protocolo

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].

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

Cell Assay^[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].

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

Animal Administration^[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.

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (280 KB)
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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Motolimod

14 Cited Publications

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Motolimod

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Publications Citing Use of MedChemExpress (MCE) Motolimod

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

Actividad biológica

Chemical Information

Publications (14)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Motolimod Related Classifications

HY-13773 Related Classifications