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盐酸伊伐布雷定 /Ivabradine HCl {[allProObj[0].p_purity_real_show]}

货号:A103870 同义名: Ivabradine (hydrochloride);S 16257

vabradine HCl 是一种 HCN (超极化激活的环核苷酸门控) 通道阻滞剂,能够抑制心脏起搏器电流 (If)。Ivabradine HCl 具有抗惊厥、抗缺血和抗心绞痛活性,可用于心率控制相关的研究和治疗。

Ivabradine HCl 化学结构 CAS号:148849-67-6
Ivabradine HCl 化学结构
CAS号:148849-67-6
Ivabradine HCl 3D分子结构
CAS号:148849-67-6
Ivabradine HCl 化学结构 CAS号:148849-67-6
Ivabradine HCl 3D分子结构 CAS号:148849-67-6
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Ivabradine HCl 纯度/质量文件 产品仅供科研

货号:A103870 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Adrenergic Receptor α-adrenergic receptor β-adrenergic receptor 其他靶点 纯度
Ivabradine HCl 98%
Maprotiline hydrochloride 98%
Cisatracurium besylate 98%
Yohimbine HCI 99+%
BMY 7378 ++

α2C-adrenoceptor, pKi: 6.54

α1D-adrenoceptor, pKi: 5.1

+

β1-adrenoceptor, pIC50: 5.1

97%
Asenapine maleate ++++

α2A-adrenergic receptor, pKi: 8.9

α2B-adrenergic receptor, pKi: 8.9

97%
Piribedil ++

adrenoceptor α2C, pKi: 7.2

adrenoceptor α2A, pKi: 7.1

98%
Prazosin HCl 95%
Silodosin 98%
Phenoxybenzamine HCl 98%
Naftopidil +++

α1A-adrenergic receptor, Ki: 3.7 nM

α1D-adrenergic receptor, Ki: 20 nM

98%
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

97%
Alfuzosin HCl 98%
Terazosin HCl 99%
Atipamezole 95%
Phentolamine methanesulfonate salt 99%
Doxazosin mesylate 98%
Tolazoline HCl 98%
Zenidolol hydrochloride ++++

β1-adrenergic receptor, Ki: 611nM

β2-adrenergic receptor, Ki: 0.7nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Ivabradine HCl 生物活性

靶点
  • Adrenergic Receptor

描述 Ivabradine Hydrochloride is a novel selective inhibitor of hyperpolarization-activated cyclic nucleotide-gated channels, inducing heart rate (HR) reduction[3]. Ivabradine at 10 mg/kg/day reduced the maximal HR increase in response to the β-agonist isoproterenol, without modifying the response of contractile parameters [4]. Ivabradine induced a time-dependent inhibition of hHCN4 with an IC50 of 0.5 μM. Ivabradine 3 μM decreased the frequency of action potentials in SAN (sino-atrial nodes) from guinea-pig, rabbit and pig by 33%, 21% and 15% at 40 min, respectively[5].

Ivabradine HCl 参考文献

[1]Lodhi M, Dubey A, et al. Formulation and evaluation of buccal film of Ivabradine hydrochloride for the treatment of stable angina pectoris. Int J Pharm Investig. 2013 Jan;3(1):47-53.

[2]Thollon C, Cambarrat C, et al. Electrophysiological effects of S 16257, a novel sino-atrial node modulator, on rabbit and guinea-pig cardiac preparations: comparison with UL-FS 49. Br J Pharmacol. 1994 May;112(1):37-42.

[3]Simko F, Baka T, Poglitsch M, Repova K, Aziriova S, Krajcirovicova K, Zorad S, Adamcova M, Paulis L. Effect of Ivabradine on a Hypertensive Heart and the Renin-Angiotensin-Aldosterone System in L-NAME-Induced Hypertension. Int J Mol Sci. 2018 Oct 3;19(10):3017.

[4]Du XJ, Feng X, Gao XM, Tan TP, Kiriazis H, Dart AM. I(f) channel inhibitor ivabradine lowers heart rate in mice with enhanced sympathoadrenergic activities. Br J Pharmacol. 2004 May;142(1):107-12.

[5]Thollon C, Bedut S, Villeneuve N, Cogé F, Piffard L, Guillaumin JP, Brunel-Jacquemin C, Chomarat P, Boutin JA, Peglion JL, Vilaine JP. Use-dependent inhibition of hHCN4 by ivabradine and relationship with reduction in pacemaker activity. Br J Pharmacol. 2007 Jan;150(1):37-46.

Ivabradine HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.90mL

1.98mL

0.99mL

19.80mL

3.96mL

1.98mL

Ivabradine HCl 技术信息

CAS号148849-67-6
分子式C27H37ClN2O5
分子量 505.05
别名 Ivabradine (hydrochloride);S 16257;Ivabradine hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

DMSO: 25 mg/mL(49.5 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 50 mg/mL(99 mM),配合低频超声助溶

动物实验配方
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