Motolimod (VTX-2337)

  Cat. No.:  DC8815   Featured
Chemical Structure
926927-61-9
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Field of application
Motolimod (VTX-2337) is a novel TLR8 agonist that activates NK cells and augments ADCC.
Cas No.: 926927-61-9
Chemical Name: 3H-1-Benzazepine-4-carboxamide, 2-amino-N,N-dipropyl-8-[4-(1-pyrrolidinylcarbonyl)phenyl
Synonyms: VTX 2337,VTX2337
SMILES: N1C2=CC(C3=CC=C(C(N4CCCC4)=O)C=C3)=CC=C2C=C(C(N(CCC)CCC)=O)CC=1N
Formula: C28H34N4O2
M.Wt: 458.6
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Motolimod is a selective Toll-like receptor 8 (TLR8) agonist, with an EC50 of approximately 100 nM.
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].
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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