| References: |
A cell-permeable, 3-acryl-acrylamide derivative that acts as a highly potent, selective, and competitive antagonist of prostaglandin E2 receptor (EP2, Kb = 17.8 nM). Exhibits about 300-fold selectivity for the EP2 receptor over human EP3, EP4, and IP receptors, about 100- fold selectivity over human EP1, 25-fold selectivity against human FP and TP, and 10-fold selectivity against human DP1 receptors. Does not affect the activity of about 40 enzymes, ion channels, receptors, and neurotransmitters even at higher concentrations (˜10 µM). Shown to significantly reduce the induction of several inflammatory cytokines and chemokines and reduces the opening of blood-brain barrier during neuronal inflammation. Displays good pharmacokinetic properties with a half-life of 1.6 h and brain to plasma ratio of 1.6 in a murine model (5 mg/kg i.p.). For the detailed information of TG6-10-1, the solubility of TG6-10-1 in water, the solubility of TG6-10-1 in DMSO, the solubility of TG6-10-1 in PBS buffer, the animal experiment (test) of TG6-10-1, the cell expriment (test) of TG6-10-1, the in vivo, in vitro and clinical trial test of TG6-10-1, the EC50, IC50,and affinity,of TG6-10-1, For the detailed information of TG6-10-1, the solubility of TG6-10-1 in water, the solubility of TG6-10-1 in DMSO, the solubility of TG6-10-1 in PBS buffer, the animal experiment (test) of TG6-10-1, the cell expriment (test) of TG6-10-1, the in vivo, in vitro and clinical trial test of TG6-10-1, the EC50, IC50,and affinity,of TG6-10-1, Please contact DC Chemicals. |
