TRIARYLMETHANE-34
TRAM-34
CAS: 289905-88-0
Molecular Formula: C22H17ClN2
TRIARYLMETHANE-34 - Names and Identifiers
TRIARYLMETHANE-34 - Physico-chemical Properties
| Molecular Formula | C22H17ClN2 |
| Molar Mass | 344.84 |
| Melting Point | 145-147°C |
| Water Solubility | Soluble in DMSO at 2mg/ml. Insoluble in water |
| Solubility | Soluble in DMSO (10 mg/ml at 40°C), ethanol (6 mg/ml at 40°C), and DMF (>25 mg/ml) |
| Appearance | solid |
| Color | off-white |
| Storage Condition | 2-8°C |
| MDL | MFCD09842562 |
| Use | TRAM-34 is a selective and potent inhibitor of the intermediate-conductance Ca2 -activated K channel (IKCa1, KCa3.1) with Kd of 20 nM, 200- to 1500-fold selective over other ion channels, and does not block cytochrome P450. |
| In vitro study | Unlike Clotrimazole, TRAM-34 selectively inhibits IKCa1 without blocking the cytochrome P450 enzyme (CYP3A4). TRAM-34 effectively inhibited the cloned IKCa1 channel in IKCa1 transfected COS-7 cells, and also inhibited the IKCad current in human T lymphocytes and T84 Cells with Kd of 20 nM and 25 nM, respectively, and 22 nM, more potent than Clotrimazole, with Kd of 70 nM, 100 nM, and 90 nM, respectively. TRAM-34 is 200 to 1500 times more selective than other ion channels, such as Kv, BKCad, SKCad, Na , CRAC and Cl-channels. TRAM-34 significantly inhibited anti-CD3 antibody or PKC activator PMA and calcium ionophore ionomycin-induced human T lymphocyte activation with IC50 of 295-910 nM and 85-830 nM, respectively. TRAM-34 (5 μm) did not inhibit the cell viability of human T lymphocytes or some cell lines. TRAM-34 significantly inhibited EGF-induced IKCa1 up-regulation and EGF-stimulated 97r5 proliferation with an IC50 of 8 nM. TRAM-34 treatment inhibits the proliferation of human endometrial carcinoma (EC) cells and blocks the EC cell cycle so that it stops at the G0/G1 phase. TRAM-34 (1-30 μm) inhibition of IKCa1 Channel resulted in inhibition of LNCaP and PC-3 prostate cancer (PCa) cell proliferation without apoptosis in a dose-dependent manner, p21Cip1 elevation and cell cycle arrest are involved in the G1 phase. Unlike Clotrimazole, TRAM-34 selectively inhibits IKCa1 without blocking the cytochrome P450 enzyme (CYP3A4). TRAM-34 effectively inhibited the cloned IKCa1 channel in IKCa1 transfected COS-7 cells, and also inhibited the IKCa d current in human T lymphocytes and T84 Cells, with K d of 20 nM, 25 nM, and 22 nM, are more effective than Clotrimazole, K d 70 nM, 100 nM, and 90 nM, respectively. TRAM-34 significantly inhibited EGF-induced IKCa1 up-regulation, and EGF-stimulated d7r5 proliferation than other ion channels, such as K v, BKCa d, SKCa d, Na TRAM-34, the IC50 was 8 nM. TRAM-34 treatment inhibits the proliferation of human endometrial carcinoma (EC) cells and blocks the EC cell cycle so that it stops at the G0/G1 phase. TRAM-34 (1-30 μm) inhibition of IKCa1 channel, leading to inhibition of LNCaP and PC-3 prostate cancer (PCa) cell proliferation without apoptosis, in a dose-dependent manner involving p21 |
| In vivo study | TRAM-34 treated mice at a channel blocking dose (0.5 mg/kg/day)500-1,000 times for 7 days without toxicity. TRAM-34 at a dose of 120 mg/kg per day in a rat model of balloon catheter injury (BCI) significantly reduced intimal proliferation by-40%. Consistent with the effect of inhibiting EC cell proliferation in vitro, TRAM-34 treatment at 30 μm slowed the progression of HEC-1-A of tumors in vivo. TRAM-34 had no toxicity when mice were treated for 7 days at a channel blocking dose (0.5 mg/kg/day) of 500-1,000 times. TRAM-34 at a dose of 120 mg/kg per day in a rat model of balloon catheter injury (BCI) significantly reduced intimal proliferation by-40%. Consistent with the effect of inhibiting EC cell proliferation in vitro, TRAM-34 treatment at 30 μm slowed the progression of HEC-1-A of tumors in vivo. |
TRIARYLMETHANE-34 - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 22 - Harmful if swallowed |
| WGK Germany | 3 |
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Spot supply
Product Name: TRAM-34 Visit Supplier Webpage Request for quotationCAS: 289905-88-0
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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