KMN-80

• Target:

  Others|||Prostaglandin Receptor

• Related Pathways:

  GPCR/G Protein|||Immunology/Inflammation|||Others

• Bioactivity:

  The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 . Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis. KMN-80 is a substituted ?-lactam (pyrrolidinone) derivative of PGE1 that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 ?M for EP3 and > 10 ?M for all other prostanoid receptors) . In functional assays it has been shown to stimulate secreted alkaline phosphatase gene reporter activity in EP4-transfected HEK293 cells with an EC50 value of 0.19 nM, demonstrating >5,000 and 50,000-fold selectivity against EP2 and TP, respectively. KMN-80 can induce the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts in vitro (EC50s = 20 and 153 nM, respectively) and exhibits favorable tolerability up to at least 10 ?M, whereas the EP4 agonist L-902,688 is highly cytotoxic at similar concentrations in these cells. KMN-80 has been used to repair calvarial defects in an in vivo rat craniomaxillofacial reconstruction model (rate of reduction in defect size equivalent to BMP-2 treated rats) and to promote bone formation in a rat incisor tooth socket model.

• Smiles:

  C(CCCCCC(O)=O)N1[C@@H](/C=C/[C@H]([C@H](CC#CCC)C)O)CCC1=O

• Molecular Formula:

  C21H33NO4

• Molecular Weight:

  363.49

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  1628759-75-0