Description
RHC-80267 (83654-05-1) inhibits DAG Lipase activity in a variety of cell types and tissues, including canine platelets, bovine adrenal chromaffin cells, human adrenal glomerulosa cells, rat thyroid lobes and pancreatic minilobules. IC50 in canine platelets is 4 μM.1
Uses
RHC-80267 is a selective inhibitor of DAG lipase, which plays an important role in the production of arachidonic acid.
Definition
ChEBI: N-[6-[[(cyclohexylideneamino)oxy-oxomethyl]amino]hexyl]carbamic acid (cyclohexylideneamino) ester is a carbamate ester and an organonitrogen compound.
General Description
Selective inhibitor of DAG lipase activity in canine platelets (IC
50 = 4 nM) and in a variety of mammalian cells. Also inhibits glucose- and carbachol-induced insulin release from intact islets. An inhibitor of Angiotensin II (Cat. No.
05-23-0101) and ATP-induced synthesis of 6-keto-prostaglandin F1α.
Biological Activity
Inhibitor of diacylglycerol lipase (IC 50 values are 1.1 and 4 μ M in rat cardiac myocytes and canine platelets respectively). Weakly inhibits phospholipases C and A 2 . Potentiates acetylcholine evoked relaxation in mesenteric arteries by the inhibition of cholinesterase activity (IC 50 = 4 μ M).
Biochem/physiol Actions
Product does not compete with ATP.
References
[1] PAUL W. MANLEY. Anthranilic Acid Amides: A Novel Class of Antiangiogenic VEGF Receptor Kinase Inhibitors[J]. Journal of Medicinal Chemistry, 2002, 45 26: 5687-5693. DOI:
10.1021/jm020899q[2] PAUL WILLIAM MANLEY. Advances in the structural biology, design and clinical development of VEGF-R kinase inhibitors for the treatment of angiogenesis[J]. Biochimica et biophysica acta. Proteins and proteomics, 2004, 1697 1: Pages 17-27. DOI:
10.1016/j.bbapap.2003.11.010[3] PAUL W. MANLEY. Anthranilic Acid Amides: A Novel Class of Antiangiogenic VEGF Receptor Kinase Inhibitors[J]. Journal of Medicinal Chemistry, 2002, 45 26: 5687-5693. DOI:
10.1021/jm020899q[4] PAUL WILLIAM MANLEY. Advances in the structural biology, design and clinical development of VEGF-R kinase inhibitors for the treatment of angiogenesis[J]. Biochimica et biophysica acta. Proteins and proteomics, 2004, 1697 1: Pages 17-27. DOI:
10.1016/j.bbapap.2003.11.010[5] PAUL W. MANLEY. Anthranilic Acid Amides: A Novel Class of Antiangiogenic VEGF Receptor Kinase Inhibitors[J]. Journal of Medicinal Chemistry, 2002, 45 26: 5687-5693. DOI:
10.1021/jm020899q
