FSL-1 (trifluoroacetate salt)

FSL-1 is a synthetic lipopeptide agonist of toll-like receptor 2 (TLR2) and TLR6 heterodimers (TLR2/TLR6). In HEK293 cells transfected with human TLR2 and TLR6 but not TLR6 alone, FSL-1 increases NF-kappaB activity by 4- and 8-fold when used at concentrations of 0.1 and 1 nM, respectively. It induces the expression of the cytokines CCL20, IL-8, IL-1beta, and TNF-alpha in human monocytic THP-1 cells and, to a lesser extent, in TLR10 knockdown cells when used at a concentration of 100 ng/ml. FSL-1 (0.5-50 µg/ml), in combination with IFN-gamma, dose-dependently increases the percentage of DM13 and VMM1 melanoma cells expressing the chemokine CXCL10 with a maximal increase of approximately 50%. In rats, FSL-1 (100 µg/kg, i.p.) induces fever and increases plasma levels of IL-6 and TNF-alpha by greater than 90-fold. FSL-1 (10-1,000 µg/kg, i.p.) also dose-dependently reduces home cage locomotor activity and both food and water consumption with maximal reductions of ten grams per 12 hours.Formal Name: S-[2,3-bis[(1-oxohexadecyl)oxy]propyl]-L-cysteinylglycyl-L-alpha-aspartyl-L-prolyl-L-lysyl-L-histidyl-L-prolyl-L-lysyl-L-seryl-L-phenylalanine, trifluoroacetate salt. Molecular Formula: C84H140N14O18S . XCF3COOH. Formula Weight: 1666.2. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: Water: 2 mg/ml. SMILES: O=C(O)[C@@H](NC([C@H](CO)NC([C@H](CCCCN)NC([C@H]1N(C([C@@H](NC([C@H](CCCCN)NC([C@@H]2CCCN2C([C@H](CC(O)=O)NC(CNC([C@@H](N)CSCC(OC(CCCCCCCCCCCCCCC)=O)COC(CCCCCCCCCCCCCCC)=O)=O)=O)=O)=O)=O)CC3=CN=CN3)=O)CCC1)=O)=O)=O)CC4=CC=CC=C4.OC(C(F)(F)F)=O. InChi Code: InChI=1S/C84H140N14O18S.C2HF3O2/c1-3-5-7-9-11-13-15-17-19-21-23-25-30-44-74(103)115-56-62(116-75(104)45-31-26-24-22-20-18-16-14-12-10-8-6-4-2)57-117-58-63(87)76(105)89-54-72(100)91-67(52-73(101)102)83(112)98-49-37-43-71(98)81(110)92-64(40-32-34-46-85)77(106)94-66(51-61-53-88-59-90-61)82(111)97-48-36-42-70(97)80(109)93-65(41-33-35-47-86)78(107)96-69(55-99)79(108)95-68(84(113)114)50-60-38-28-27-29-39-60,3-2(4,5)1(6)7/h27-29,38-39,53,59,62-71,99H,3-26,30-37,40-52,54-58,85-87H2,1-2H3,(H,88,90)(H,89,105)(H,91,100)(H,92,110)(H,93,109)(H,94,106)(H,95,108)(H,96,107)(H,101,102)(H,113,114),(H,6,7)/t62?,63-,64-,65-,66-,67-,68-,69-,70-,71-,/m0./s1. InChi Key: UANJOAKJMWZEBV-ALAVPRNSSA-N.