85-2076-51　RXFP1 Agonist (2-Isopropoxy-N-(2-(3-(trifluoromethylsulfonyl)phenylcarbamoyl)phenyl)benzamide, LGR7 Agonist, Relaxin/Insulin-like Family Peptide Receptor 1 Agonist, Leucine-Rich Repeat-Containing GPCR 7 Agonist) 10mg　217762

特徴

• A cell-permeable 2-acetamido-N-phenylbenzamide that selectively activates human, but not mouse, LGR7/RXFP1-mediated cAMP induction (EC50 = 200nM in THP1) via allosteric interaction with the ECL3 region without competing against ECL2-mediated relaxin binding or affecting AVPR1B- or LGR8/RXFP2-mediated cAMP induction. Although shown to be ~150-fold and 500-fold less potent than relaxin (RLX), respectively, in VEGF mRNA induction and cellular impedance assays, pharmacokinetic studies reveal superior in vivo stability to RLX and in vivo bioavailability in mice via oral (Cmax/Tmax = 604nM/plasma/1h and 1026ng/g heart/1.5h; 30mg/kg) or intraperitoneal (Cmax/Tmax = 9.29uM/plasma/1h and 28.6uMol/kg heart/1h; 30mg/kg) administration with good aqueous solubility (7uM in PBS).
• Synonyms:Leucine-Rich Repeat-Containing GPCR 7 Agonist, LGR7 Agonist, Relaxin/Insulin-like Family Peptide Receptor 1 Agonist, 2-Isopropoxy-N-(2-(3-(trifluoromethylsulfonyl)phenylcarbamoyl)phenyl)benzamide
• Formula:C₂₄H₂₁F₃N₂O₅S
• Solubility:DMSO (50mg/ml)
• Primary Target:hRXFP1
• Storage and Stability:Store at 4°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.