TRPP3, a member of the transient receptor potential (TRP) superfamily of cation channels, is a Ca-activated channel permeable to Ca, Na, and K. TRPP3 is implicated in regulation of pH-sensitive action potential in spinal cord neurons.
Phenamil methanesulfonate (1 μM) decreases Ca uptake in a radiotracer uptake assay. It inhibits TRPP3-mediated Ca transport with an IC50 value of 0.28 μM in oocytes expressing TRPP3 or H2O-injected oocytes.
Phenamil methanesulfonate is a more potent ENaC blocker than Amiloride, it inhibits the epithelial sodium channel (ENaC) with an IC50 of 400 nM (Amiloride=776 nM).
Phenamil methanesulfonate inhibits basal short-circuit currents with IC50 values of 75 and 116 nM, respectively in both human and ovine bronchial epithelia cells.
Phenamil methanesulfonate (0-20 μM; 14 days) elevates adipogenic gene expression, PPARγ, Fabp4, and lipoprotein lipase expression in a concentration-dependent manner ,and regulates adipogenesis in C3H10T1/2 cells.
Phenamil methanesulfonate (0-20 μM; 7 or 14 days) modulates MC3T3-E1 osteoblastic differentiation, it increases Alkaline phosphatase (ALP) activity in MC3T3-E1 cells in a concentration-dependent manner.
RT-PCR
Cell Line: |
C3H10T1/2 cells |
Concentration: |
0 μM and 20 μM |
Incubation Time: |
14 days |
Result: |
Increased PPARγ, Fabp4, and lipoprotein lipase (LPL) mRNA expression. |