Motolimod 是一种有效且特异性的 Toll 样受体 8 (TLR8) 激动剂，EC50约为 100 nM。

Motolimod (VTX-2337) is an effective and specific Toll-like receptor (TLR) 8 agonist (EC50: 100 nM), >50-fold selectivity over TLR7.

VTX-2337 induces the production of both TNFα (EC50: 140 nM) and IL-12 (EC50: 120 nM) in PBMCs. In mDCs and monocytes, VTX-2337 specifically induces the production of IL-12 and TNFα via NF-κB activation. VTX-2337 also induces IFNγ production from NK cells, enhances the lytic function of NK cells and augments ADCC.

In ovarian cancer mouse model, TX-2337 augments the effect of pegylated liposomal doxorubicin (PLD).

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.

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.

926927-61-9

C28H34N4O2

458.606

VTX-378;VTX-2337

DMSO:51 mg/mL (111.2 mM)
H2O:<1 mgml
Ethanol:12 mg/mL (26.2 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years