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KRN4884

MCE 国际站：KRN4884

品牌：MedChemExpress (MCE)

货号：HY-U00201

CAS 号：152802-84-1

生物活性：KRN4884 是一种 K+ 通道开放剂。在细胞内 ATP (1 mM) 存在的情况下，KRN4884 (0.1-3 μM) 以浓度依赖的方式激活 KATP 通道 (EC50=0.55 μM)。

体外研究(In Vitro)：KRN4884 (0.3 μM) shifts the concentration-response relationship for ATP-induced KATP channel inhibition to the right and slightly upward direction without altering the slope. After either the spontaneous or Ca2+-induced channel rundown, KRN4884 (1 and 3 μM) partially restores the KATP channel activity. Furthermore, the effect of KRN4884 is augmented by the presence of uridine 5′-diphosphate (3 mM). KRN4884 activates cardiac KATP channels through not only decreasing the sensitivity of the channel to ATP but also directly stimulating the opening of the channel. KRN4884 (0.3 and 3 μM) increases the outward current in a concentration-dependent manner, and the unitary current amplitudes are similar to that of KATP channels in the ATP-free solution[1]. MCE尚未独立确认这些方法的准确性。 仅供参考。

体内研究(In Vivo)：The effects of KRN4884, a novel pyridinecarboxamidine type KATP channel opener, on serum triglyceride levels are investigated in Sprague-Dawley rats. Oral administration of KRN4884 (3 mg/kg) for 10 days causes a significant reduction in serum triglyceride levels, which is comparable to that of Clofibrate (160 mg/kg). Reduction in serum triglyceride levels by KRN4884 and Clofibrate are accompanied by a reduction in triglyceride levels both in chylomicron and in very low density lipoprotein. KRN4884 treatment does not affect serum concentrations of total cholesterol and phospholipid, but increases free fatty acid levels. Rats receiving KRN4884 exhibite an increase in lipoprotein lipase (LPL) activity both in adipose tissue and in skeletal muscle[2]. MCE尚未独立确认这些方法的准确性。 仅供参考。

分子量：299.76

Formula：C15H14ClN5

运输条件：美国大陆地区的室温；其他地区可能有所不同。

储存方式：请按照分析证书中推荐的条件储存产品。

Kinase Assay [1]： KRN4884 以 10 mM 的浓度溶于 DMSO 中配制成储备液，并用灌流液稀释。细胞最终接触的 DMSO 浓度低于 0.1%[1]。为了定量分析 KRN4884 或其他化合物的作用，通道活性以 NPoi 表示。NPoi 的计算方法是：在每种药物的稳态作用期间，对 5 至 15 秒的连续电流记录进行积分。KRN4884 的浓度-反应曲线是通过将 NPoi 值归一化到用不含 ATP 的灌流液灌注所获得的 NPoi 值，并拟合 Hill 方程得到的[1]。MCE 尚未独立确认这些方法的准确性。仅供参考。

Animal Administration [2]：Rats[2] Five-week old male Sprague-Dawley (Crj; CD) rats are obtained and housed in a temperature-controlled environment with a 12 h daily light cycle with free access to water and chow (CE-2). At 6-weeks old, the animals are assigned to vehicle, Clofibrate (160 mg/kg) or KRN4884 (3 mg/kg) treatment groups. The drug is given daily, by gavage for 10 days at 2 mL/kg as a suspension in 0.5% (w/v) carboxymethyl cellulose. Systolic blood pressure is determined 1 h after administration on day 9 with the tail cu. method by use of a sphygmomanometer. Four hours after the final administration of the drug or vehicle on day 10, non-fasting blood is collected from an abdominal aorta of each rat under ether anaesthesia. Serum is provided for lipid analysis. Epididymal adipose tissue, thigh muscle, and liver are removed and weighed, then immediately immersed in liquid nitrogen and stored at -80°C until use. Epididymal adipose tissue and thigh muscle are used for determining lipoprotein lipase (LPL) activity and the liver is used for de- termining hepatic triglyceride lipase (HTGL) activity. MCE尚未独立确认这些方法的准确性。 仅供参考。

提供质量检测报告：Data Sheet、产品使用指南

产品活性：KRN4884 是一种 K+ 通道开放剂。在细胞内 ATP (1 mM) 存在下，KRN4884 (0.1-3 μM) 激活 KATP通道 (EC50=0.55 μM), 这种作用存在浓度依赖性。

IC50 & Target：EC50: 0.55 μM (KATP channel)[1]

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客户发表文献：
[1]. Nature. 2026 Sep;657(8131):549-558.
[2]. Nature. 2026 Sep;657(8132):755-764.
[3]. Nature. 2026 Sep;657(8133):1027-1034.
[4]. Nature. 2026 Sep;657(8131):477-486.
[5].Nature. 2026 Sep;657(8132):789-799.
[6]. Nature. 2026 Sep;657(8131):517-524.
[7]. Nature. 2026 Sep;657(8133):1045-1052.
[8]. Cell. 2026 Sep 14:S0092-8674(26)01003-2.
[9]. Cell. 2026 Sep 3;189(18):5688-5705.e13.
[10]. Cell. 2026 Sep 2:S0092-8674(26)00937-2.

参考文献：
[1]. Shinbo A, et al. Activation of cardiac ATP-sensitive K+ channels by KRN4884, a novel K+ channel opener. J Pharmacol Exp Ther. 1997 Nov;283(2):770-7.
[2]. Yokoyama T, et al. Effects of KRN4884, a novel pyridinecarboxamidine type KATP channel opener, on serum triglyceride levels in rats. Br J Pharmacol. 1997 Apr;120(8):1471-6.