Ivabradine HCl

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Chemical Structure| 148849-67-6 同义名 : Ivabradine (hydrochloride);S 16257;Ivabradine hydrochloride
CAS号 : 148849-67-6
货号 : A103870
分子式 : C27H37ClN2O5
纯度 : 98%
分子量 : 505.05
MDL号 : MFCD00929899
存储条件：

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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.