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TRAM-34

TRAM-34

产品编号 T6186   CAS 289905-88-0
别名: Triarylmethane-34, TRAM 34

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。

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TRAM-34 Chemical Structure
TRAM-34, CAS 289905-88-0
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
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: TRAM-34 (T6186)
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纯度: 99.76%
纯度: 99.01%
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 3.5 mg/mL (10 mM), Heating is recommended.

溶液配制表

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

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TargetMol Library Books参考文献

1. Wulff H, et al. Proc Natl Acad Sci U S A, 2000, 97(14), 8151-8156. 2. Köhler R, et al. Circulation, 2003, 108(9), 1119-1125. 3. Wang ZH, et al. Oncogene, 2007, 26(35), 5107-5114. 4. Lallet-Daher H, et al. Oncogene, 2009, 28(15), 1792-1806.
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相关化合物库

该产品包含在如下化合物库中:
抑制剂库 HIF-1化合物库 NO PAINS 化合物库 抗乳腺癌化合物库 免疫/炎症分子化合物库 已知活性化合物库 离子通道库 抗卵巢癌化合物库 抗癌化合物库 抗肝癌化合物库

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Keywords

TRAM-34 289905-88-0 Membrane transporter/Ion channel NF-Κb Potassium Channel IκB/IKK Triarylmethane-34 Inhibitor KcsA inhibit TRAM34 TRAM 34 inhibitor

 

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