Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TRAM-34 (Triarylmethane-34) 是一种高选择性的钙激活 K+通道 (IKCa1)阻断剂,Kd 值为 20 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 233 | 现货 | ||
5 mg | ¥ 396 | 现货 | ||
10 mg | ¥ 619 | 现货 | ||
25 mg | ¥ 1,230 | 现货 | ||
50 mg | ¥ 1,990 | 现货 | ||
100 mg | ¥ 3,660 | 现货 | ||
200 mg | ¥ 5,220 | 现货 | ||
500 mg | ¥ 7,890 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 422 | 现货 |
产品描述 | TRAM-34 (Triarylmethane-34) (Kd=20 nM), an effective and specific inhibitor of the intermediate-conductance Ca2+-activated K+ channel (IKCa1, KCa3.1), does not block cytochrome P450. The selective activity of TRAM-34(TRAM 34) is 200 to 1500-fold than other ion channels. |
靶点活性 | IKCa1:20 nM (Kd) |
体外活性 | Unlike clotrimazole, TRAM-34 selectively inhibits IKCa1 without blocking cytochrome P450 enzyme (CYP3A4). TRAM-34 potently inhibits cloned IKCa1 channel in IKCa1-transfected COS-7 cells as well as native IKCa currents in human T lymphocytes and T84 cells with Kd of 20 nM, 25 nM, and 22 nM, respectively, more potently than clotrimazole with Kd of 70 nM, 100 nM, and 90 nM, respectively. TRAM-34 exhibits 200- to 1,500-fold selectivity over other ion channels such as KV, BKCa, SKCa, Na+, CRAC, and Cl- channels. TRAM-34 significantly inhibits anti-CD3 Ab or PKC-activator PMA plus calcium-ionophore ionomycin-induced activation of human T lymphocytes with IC50 of 295-910 nM and 85-830 nM, respectively. TRAM-34 (5 μM) does not inhibit cell viability of human T lymphocytes or several cell lines. [1] TRAM-34 significantly inhibits EGF-induced IKCa1 up-regulation, and EGF-stimulated proliferation of A7r5 cells with IC50 of 8 nM. [2] TRAM-34 treatment inhibits proliferation of human endometrial cancer (EC) cells and blocks EC cell cycle at G0/G1 phase. [3] |
体内活性 | TRAM-34 treatment at ~500-1,000 times the channel-blocking dose (0.5 mg/kg/day) for 7 days is nontoxic to mice. [1] Administration of TRAM-34 at 120 mg/kg/day significantly reduces intimal hyperplasia by ~40% in a rat model of balloon catheter injury (BCI). [2] Consistent with it's in vitro role in inhibiting the proliferation of EC cells, TRAM-34 treatment at 30 μM slows the development of HEC-1-A tumor in vivo. [3] |
激酶实验 | Electrophysiology: The human IKCa1 is cloned and expressed in COS-7 cells. Cells are studied in the whole-cell configuration of the patch-clamp technique. The holding potential is 280 mV. The internal pipette solution contains: 145 mM K+ aspartate, 2 mM MgCl2, 10 mM Hepes, 10 mM K2EGTA, and 8.5 mM CaCl2 (1 μM free Ca2+), pH 7.2, 290-310 mOsm. To reduce currents from the native chloride channels in COS-7 cells, Na+ aspartate Ringer is used as an external solution: 160 mM Na+ aspartatey/4.5 mM KCl/2 mM CaCl2/1 mM MgCl2/5 mM Hepes, pH 7.4/290-310 mOsm. IKCa currents in COS-7 cells are elicited by 200-ms voltage ramps from -120 mV to 40 mV applied every 10 seconds and the reduction of slope conductance at -80 mV by TRAM-34 taken as a measure of channel block. |
细胞实验 | Cells are exposed to TRAM-34 for 48 hours. After 48 hours, 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 red fluorescence measured on a FACScan flow cytometer. The percentage of dead cells is determined by their PI uptake, 104 cells of every sample being analyzed. (Only for Reference) |
别名 | Triarylmethane-34, TRAM 34 |
分子量 | 344.84 |
分子式 | C22H17ClN2 |
CAS No. | 289905-88-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 3.5 mg/mL (10 mM), Heating is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.8999 mL | 14.4995 mL | 28.999 mL | 72.4974 mL |
5 mM | 0.58 mL | 2.8999 mL | 5.7998 mL | 14.4995 mL | |
10 mM | 0.29 mL | 1.4499 mL | 2.8999 mL | 7.2497 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
TRAM-34 289905-88-0 Membrane transporter/Ion channel NF-Κb Potassium Channel IκB/IKK Triarylmethane-34 Inhibitor KcsA inhibit TRAM34 TRAM 34 inhibitor