Home Immunology & Inflammation TLR agonist Motolimod For research use only.

Motolimod

Synonyms: VTX-2337

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

Motolimod Chemical Structure

Motolimod Chemical Structure

CAS No. 926927-61-9

Purity & Quality Control

Batch: S716101 DMSO]55 mg/mL]false]Ethanol]15 mg/mL]false]Water]Insoluble]false Purity: 99.80%
99.80

Motolimod Related Products

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
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]
Kinase Assay 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 Research 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.
In Vivo
In vivo In an ovarian cancer mouse model, TX-2337 enhances the effect of pegylated liposomal doxorubicin (PLD). [2]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03906526 Terminated
Carcinoma Squamous Cell
Celgene
 July 3 2019 Phase 1
NCT01289210 Terminated
Low Grade B Cell Lymphoma
Celgene|Stanford University
 July 2011 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 458.6 Formula

C28H34N4O2
CAS No. 926927-61-9 SDF Download Motolimod SDF
Smiles CCCN(CCC)C(=O)C1=CC2=C(C=C(C=C2)C3=CC=C(C=C3)C(=O)N4CCCC4)N=C(C1)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 55 mg/mL ( (119.93 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 15 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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