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TRAM-34 is a selective and potent inhibitor of the intermediate-conductance Ca2+-activated K+ channel (IKCa1, KCa3.1) with Kd of 20 nM. Unlike clotrimazole, TRAM-34 dose not inhibit mammalian cytochrome P450 enzyme (CYP3A4). TRAM-34 displays >200-fold selectivity for IKCa1 over Kv, BKCa, SKCa, Na, CRAC, and chloride channels. TRAM-34 does not exhibit toxicity against a variety of cell lines in vitro or cause obvious deleterious changes in a limited short-term acute toxicity study in rodents. TRAM-34 significantly inhibits the reactivation process of human lymphocytes by mitogenic stimuli, and when in combination with cyclosporin A suppresses T-cell mitogenesis more potently than either compound alone. TRAM-34 significantly inhibits EGF-induced IKCa1 up-regulation, and EGF-stimulated proliferation of A7r5 cells. TRAM-34 treatment at 120 mg/kg/day significantly reduces intimal hyperplasia in rat model of balloon catheter injury (BCI). TRAM-34 inhibits human endometrial cancer (EC) cell proliferation, arrests its cell cycle at G0/G1 phase, and suppresses the development of EC tumors in nude mice. By specifically targeting IKCa1, TRAM-34 treatment inhibits the prostate cancer (PCa) cell proliferation in a dose-dependent manner, involving growth arrest and an accumulation of p21Cip1.
| Cell Experiment | |
|---|---|
| Cell lines | Human T lymphocytes, Jurkat E6-1, MEL, C2F3, CHO, COS-7, L929, NGP, NLF, and RBL-2H3 |
| Preparation method | Exposing cells to TRAM-34 for 48 hours. 48 hours later , cells are harvested by suction (suspension cells) or by trypsinization (adherent cell lines), centrifuged, resuspended in 0.5 mL PBS containing 1 μg/mL propidium iodide (PI), and measured red fluorescence on a FACScan flow cytometer. The percentage of dead cells is determined by their PI uptake, 104 cells of every sample being analyzed. |
| Concentrations | Dissolved in DMSO, final concentration ~10 μM |
| Incubation time | 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | Sprague-Dawley rats subjected to BCI of the left CA by use of a 2F Fogarty embolectomy catheter |
| Formulation | Formulated in peanut oil |
| Dosages | 120 mg/kg/day |
| Administration | Subcutaneous injection |
| Molecular Weight | 344.84 |
| Formula | C22H17ClN2 |
| CAS Number | 289905-88-0 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[5] Tom Schilling, et al. TRAM-34 inhibits nonselective cation channels
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