Motolimod

Catalog No.S7161 Batch:S716101

Technical Data

Formula	C₂₈H₃₄N₄O₂
Molecular Weight	458.6	CAS No.	926927-61-9
Solubility (25°C)*	In vitro	DMSO	55 mg/mL (119.93 mM)
		Ethanol	15 mg/mL (32.7 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Motolimod is a selective and potent Toll-like receptor 8 (TLR8) agonist with EC50 of 100 nM, > 50-fold selectivity over TLR7. Phase 2.

Targets

TLR8 ^[1]

100 nM(EC50)

In vitro

VTX-2337 stimulates the production of both TNFα with EC50 of 140 nM and IL-12 with EC50 of 120 nM in PBMCs. In monocytes and mDCs, VTX-2337 selectively induces the production of TNFα and IL-12 via NF-κB activation. VTX-2337 also stimulates IFNγ production from NK cells, augments the lytic function of NK cells and enhances ADCC. ^[1]

In vivo

In an ovarian cancer mouse model, TX-2337 enhances the effect of pegylated liposomal doxorubicin (PLD). ^[2]

Protocol (from reference)

Kinase Assay:^{^[1]}	Activity assay 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 (InvivoGen) after TLR agonist treatment is carried out.
Cell Assay:^{^[1]}	Cell lines PBMCs or purified NK cells Concentrations ~500 nM Incubation Time 48 h Method PBMCs or purified NK cells are prepared as previously described, and the purity of NK cells was 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 VTX-2337 (167 or 500 nmol/L) before incubation with target cells.

Kinase Assay:^{^[1]}

Activity assay
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 (InvivoGen) after TLR agonist treatment is carried out.

Cell Assay:^{^[1]}

Cell lines
PBMCs or purified NK cells
Concentrations
~500 nM
Incubation Time
48 h
Method
PBMCs or purified NK cells are prepared as previously described, and the purity of NK cells was 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 VTX-2337 (167 or 500 nmol/L) before incubation with target cells.

References

Selleck's Motolimod has been cited by 10 publications

Preclinical Evidence for the Glucocorticoid-Sparing Potential of a Dual Toll-Like Receptor 7/8 Inhibitor in Autoimmune Diseases [ J Pharmacol Exp Ther, 2024, 388(3):751-764]	PubMed: 37673681
Induction of OCT2 contributes to regulate the gene expression program in human neutrophils activated via TLR8 [ Cell Rep, 2021, 35(7):109143]	PubMed: 34010659
Human Neutrophils Activated by TLR8 Agonists, With or Without IFNγ, Synthesize and Release EBI3, but Not IL-12, IL-27, IL-35, or IL-39 [ J Leukoc Biol, 2020, 1]	PubMed: 32480433
Determination of motolimod concentration in rat plasma by liquid chromatography-tandem mass spectrometry and its application in a pharmacokinetic study. [ J Pharm Biomed Anal, 2020, 179:112987]	PubMed: 31761376
TLR7 and TLR8 Differentially Activate the IRF and NF-κB Pathways in Specific Cell Types to Promote Inflammation. [ Immunohorizons, 2020, 4(2):93-107]	PubMed: 32086319
Activation of type I interferon antiviral response in human neural stem cells. [ Stem Cell Res Ther, 2019, 10(1):387]	PubMed: 31843025
Human neutrophils activated via TLR8 promote Th17 polarization through IL-23. [ J Leukoc Biol, 2019, 105(6):1155-1165]	PubMed: 30817049
EV71 Infection Induces IFNβ Expression in Neural Cells. [ Viruses, 2019, 11(12)]	PubMed: 31817126
TLR7/8-agonist-loaded Nanoparticles Promote the Polarization of Tumour-Associated Macrophages to Enhance Cancer Immunotherapy [ Nat Biomed Eng, 2018, 2(8):578-588]	PubMed: 31015631
The anticancer effect of mebendazole may be due to M1 monocyte/macrophage activation via ERK1/2 and TLR8-dependent inflammasome activation. [ Immunopharmacol Immunotoxicol, 2017, 39(4):199-210]	PubMed: 28472897

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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