公告提醒:爱必信所有产品和服务仅用于科学研究,不用于临床应用及其他用途提供产品和服务(也不为任何个人提供产品和服务)!

抑制剂描述:

产品名称:TRAM-34

产品别名:见爱必信官网

英文别名:TRAM-34

靶点:Potassium Channel

CAS:289905-88-0

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

TRAM-34是中电导的钙激活的钾离子通道(KCa3.1),Kd为20 nM,不抑制细胞色素P450。

溶解性:DMSO : 3.5 mg/mL (10 mM), with gentle warming

体外研究:

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. TRAM-34 significantly inhibits EGF-induced IKCa1 up-regulation, and EGF-stimulated proliferation of A7r5 cells with IC50 of 8 nM. TRAM-34 treatment inhibits proliferation of human endometrial cancer (EC) cells, and blocks EC cell cycle at G0/G1 phase. Inhibition of the IKCa1 channel by TRAM-34 (1-30 μM) leads to dose-dependent suppression of the proliferation but not apoptosis of LNCaP and PC-3 prostate cancer (PCa) cells, involving an increase of p21Cip1 and cell arrest in the G1 cycle.

体内研究:TRAM-34 treatment at ~500-1,000 times the channel-blocking dose (0.5 mg/kg/day) for 7 days is nontoxic to mice. Administration of TRAM-34 at 120 mg/kg/day significantly reduces intimal hyperplasia by ~40% in a rat model of balloon catheter injury (BCI). Consistent with its 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.

产品信息订购:

产品更多信息请进入爱必信网站咨询