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  • TRAM-34

    • TRAM34; TRAM 34; Triarylmethane-34
    货号: abs812222
    CAS号: 289905-88-0
    分子式: C22H17ClN2
    分子量: 344.84
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    货号-规格 货期 价格 数量
    abs812222-5mg 1-2周 ¥582.00
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    abs812222-10mg 现货 ¥933.00
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    abs812222-50mg 现货 ¥2850.00
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    大包装询价
    产品描述
    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。

    纯度
    >98%
    储存/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.
    基本信息
    别名
    TRAM34; TRAM 34; Triarylmethane-34
    外观
    白色粉末
    可溶性/溶解性
    DMSO : 3.5 mg/mL (10 mM), with gentle warming
    生物活性
    靶点
    IKCa1 (KCa3.1)
    In vitro(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.
    In vivo(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.
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    参考文献
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