Motolimod

Motolimod is an agonist of toll-like receptor 8 (TLR8). It increases the production of TNF-alpha and IL-12 in human peripheral blood mononuclear cells (PBMCs, EC50s = 140 and 120 nM, respectively), monocytes, and myeloid dendritic cells. Motolimod also increases IFN-gamma production in natural killer (NK) cells and increases cytolysis in K562 NK cell-sensitive leukemia cells when used at concentrations of 167 and 500 nM for 48 hours. It increases plasma levels of a group of human cytokines, including IL-6, IL-12p70, TNF-alpha, MCP-1, and MIP-1beta, in NOD-scid IL2rynull (NSG) mice reconstituted with human immune system (NSG-HIS) when administered at doses of 1.5 and 15 mg/m2. Motolimod, when used in combination with pegylated liposomal doxorubicin (PLD), reduces tumor growth and increases tumor infiltration of monocytes and T cells in an ovarian cancer NSG-HIS mouse model.Formal Name: 2-amino-N,N-dipropyl-8-[4-(1-pyrrolidinylcarbonyl)phenyl]-3H-1-benzazepine-4-carboxamide. CAS Number: 926927-61-9. Synonyms: VTX-2337. Molecular Formula: C28H34N4O2. Formula Weight: 458.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 2 mg/ml, DMSO:PBS (pH 7.2) (1:4): 0.20 mg/ml. lambdamax: 270 nm. SMILES: O=C(N1CCCC1)C(C=C2)=CC=C2C3=CC(N=C(N)CC(C(N(CCC)CCC)=O)=C4)=C4C=C3. InChi Code: InChI=1S/C28H34N4O2/c1-3-13-31(14-4-2)28(34)24-17-23-12-11-22(18-25(23)30-26(29)19-24)20-7-9-21(10-8-20)27(33)32-15-5-6-16-32/h7-12,17-18H,3-6,13-16,19H2,1-2H3,(H2,29,30). InChi Key: QSPOQCXMGPDIHI-UHFFFAOYSA-N.