Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ivabradine hydrochloride (S 16257-2) 是一种可口服的,超极化激活的环核苷酸门控离子通道通道阻滞剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
10 mg | ¥ 280 | 现货 | ||
25 mg | ¥ 446 | 现货 | ||
50 mg | ¥ 622 | 现货 | ||
100 mg | ¥ 913 | 现货 | ||
200 mg | ¥ 1,370 | 现货 | ||
500 mg | ¥ 2,290 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 446 | 现货 |
产品描述 | Ivabradine hydrochloride (S 16257-2) is a new If inhibitor (IC50: 2.9 μM). Ivabradine Hydrochloride is the hydrochloride salt form of ivabradine, an orally bioavailable, hyperpolarization-activated, cyclic nucleotide-gated (HCN) channel blocker, with negative chronotropic activity. Upon administration, ivabradine selectively binds to the intracellular portion of the HCN channel pore and blocks HCN channels in the pacemaker cells within the sinoatrial (SA) node. This inhibits the If (funny) pacemaker ion current, prevents the inward flow and intracellular accumulation of positively charged ions, reduces pacemaker activity and slows diastolic depolarization. |
靶点活性 | If:2.9 μM |
体内活性 | Ivabradine treatment (10 mg/kg/d) induces long-term HRR, and that improves diastolic LV function probably involving attenuated hypoxia, reduced remodeling, and/or preserved nitric oxide bioavailability, resulting from processes triggered early after HRR initiation: angiogenesis and/or preservation of endothelial nitric oxide synthase expression[1]. Ivabradine causes a sustained 15-20% heart rate reduction, but has no effect on blood pressure. While ivabradine has no effect on endothelial function and vascular reactive oxygen species production in angiotensin II-treated rats, it improves both parameters in ApoE knockout mice. Ivabradine treatment leads to an attenuation of angiotensin II signaling and increased the expression of telomere-stabilizing proteins in ApoE knockout mice, which may explain its beneficial effects on the vasculature. The absence of these protective ivabradine effects in angiotensin II-infused rats may relate to the treatment duration or the presence of arterial hypertension[2]. |
别名 | 盐酸伊伐布雷定, S 16257-2, Ivabradine HCl |
分子量 | 505.05 |
分子式 | C27H37ClN2O5 |
CAS No. | 148849-67-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (184.1 mM)
Ethanol: 93 mg/mL (184.1 mM)
H2O: 75 mg/mL (148.5 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol / H2O | 1 mM | 1.98 mL | 9.9 mL | 19.8 mL | 49.5 mL |
5 mM | 0.396 mL | 1.98 mL | 3.96 mL | 9.9 mL | |
10 mM | 0.198 mL | 0.99 mL | 1.98 mL | 4.95 mL | |
20 mM | 0.099 mL | 0.495 mL | 0.99 mL | 2.475 mL | |
50 mM | 0.0396 mL | 0.198 mL | 0.396 mL | 0.99 mL | |
100 mM | 0.0198 mL | 0.099 mL | 0.198 mL | 0.495 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。
Ivabradine hydrochloride 148849-67-6 GPCR/G Protein Neuroscience Adrenergic Receptor heart rate orally active anticonvulsant Inhibitor 盐酸伊伐布雷定 Ivabradine Ivabradine Hydrochloride anti-ischaemic anti-anginal inhibit Hyperpolarization activated cyclic nucleotide gated channels S 16257-2 HCN Channel Ivabradine HCl inhibitor