ICI 118,551 hydrochloride
(Synonyms: ICI 118551 hydrochloride) 目录号 : GC14033
ICI 118,551 hydrochloride是一种选择性β2-肾上腺素受体拮抗剂。
Cas No.:72795-01-8
Sample solution is provided at 25 µL, 10mM.
ICI 118,551 hydrochloride is a selective β2-adrenergic receptor antagonist [1]. By competitively blocking β2-adrenergic receptors, ICI 118,551 hydrochloride inhibits epinephrine- or norepinephrine-mediated signal transduction, thereby affecting β2-receptor-related physiological processes in the cardiovascular and respiratory systems [2-3]. ICI 118,551 hydrochloride is commonly used to treat heart failure [4].
In HeLa 9xHRE-Luc cell, ICI 118,551 hydrochloride (0–200μM; 24h) decreases viability in hemangioblastomas by inducing cell apoptosis [5]. In induced pluripotent stem cells, ICI 118,551 hydrochloride (0.3μM; 30min) pretreatment of cells significantly inhibited the increase in KDR expression induced by L-isoproterenol [6]. In BxPC-3 and MIA PaCa-2 cells, ICI 118,551 hydrochloride (1-100μM; 24h) enhanced the antiproliferative and proapoptotic effects induced by gemcitabine [7].
In 3xTg-alzheimer's disease (AD) mice, ICI 118,551 hydrochloride (1 mg/kg; ip; 45 days) exacerbates cognitive deficits in the AD mouse model [8]. In wild-type mice, ICI 118,551 hydrochloride (0.7mg/kg; iv; 14d) increases PKA activity [9].
References:
[1]. Billman G E, Castillo L C, Hensley J, et al. β2-Adrenergic receptor antagonists protect against ventricular fibrillation: in vivo and in vitro evidence for enhanced sensitivity to β2-adrenergic stimulation in animals susceptible to sudden death[J]. Circulation, 1997, 96(6): 1914-1922.
[2]. Denda M, Fuziwara S, Inoue K. β2-adrenergic receptor antagonist accelerates skin barrier recovery and reduces epidermal hyperplasia induced by barrier disruption[J]. Journal of Investigative Dermatology, 2003, 121(1): 142-148.
[3]. Boshchenko A A, Kurbatov B K, Kilin M, et al. Role of β-Adrenergic Receptors in Stress-Induced Cardiac Injury[J]. Bulletin of Experimental Biology and Medicine, 2025: 1-4.
[4]. Gong H, Sun H, Koch W J, et al. Specific β2AR blocker ICI 118,551 actively decreases contraction through a Gi-coupled form of the β2AR in myocytes from failing human heart[J]. Circulation, 2002, 105(21): 2497-2503.
[5]. Cuesta A M, Albiñana V, Gallardo-Vara E, et al. The β2-adrenergic receptor antagonist ICI-118,551 blocks the constitutively activated HIF signalling in hemangioblastomas from von Hippel-Lindau disease[J]. Scientific reports, 2019, 9(1): 10062.
[6]. Ishizuka T, Goshima H, Ozawa A, et al. Involvement of β-adrenoceptors in the differentiation of human induced pluripotent stem cells into mesodermal progenitor cells[J]. European Journal of Pharmacology, 2014, 740: 28-34.
[7]. Shan T, Ma Q, Zhang D, et al. β2-adrenoceptor blocker synergizes with gemcitabine to inhibit the proliferation of pancreatic cancer cells via apoptosis induction[J]. European journal of pharmacology, 2011, 665(1-3): 1-7.
[8]. Branca C, Wisely E V, Hartman L K, et al. Administration of a selective β2 adrenergic receptor antagonist exacerbates neuropathology and cognitive deficits in a mouse model of Alzheimer's disease[J]. Neurobiology of aging, 2014, 35(12): 2726-2735.
[9]. Liu X, Callaerts-Vegh Z, Evans K L J, et al. Chronic infusion of β-adrenoceptor antagonist and inverse agonists decreases elevated protein kinase A activity in transgenic mice with cardiac-specific overexpression of human β2-adrenoceptor[J]. Journal of cardiovascular pharmacology, 2002, 40(3): 448-455.
ICI 118,551 hydrochloride是一种选择性β2-肾上腺素受体拮抗剂 [1]。通过竞争性阻断β2-肾上腺素受体，ICI 118,551 hydrochloride抑制肾上腺素或去甲肾上腺素介导的信号转导，从而影响心血管和呼吸系统中与β2受体相关的生理过程 [2-3]。ICI 118,551 hydrochloride常用于治疗心力衰竭 [4]。
在HeLa 9xHRE-Luc细胞中，ICI 118,551 hydrochloride（0-200μM；24 h）通过诱导细胞凋亡降低血管母细胞瘤的存活率 [5]。在诱导性多能干细胞中，ICI 118,551 hydrochloride（0.3μM；30min）预处理细胞可显著抑制L-异丙肾上腺素诱导的KDR表达增加 [6]。在BxPC-3和MIA PaCa-2细胞中，ICI 118,551 hydrochloride（1-100μM；24h）可增强吉西他滨诱导的抗增殖和促凋亡作用 [7]。
在3xTg-阿尔茨海默症（AD）小鼠中，ICI 118,551 hydrochloride（1mg/kg；ip；45d）会加剧AD小鼠模型的认知缺陷 [8]。在野生型小鼠中，ICI 118,551 hydrochloride（0.7mg/kg；iv；14d）可提高PKA活性 [9]。
| Cell experiment [1]: | |
Cell lines | HeLa 9xHRE-Luc cell |
Preparation Method | 5 × 103 cells were seeded in 96-well/plates and cultured in 100 μl with increasing doses [0–200μM] of Atenolol, or Propranolol, or ICI 118,551 hydrochloride for the time indicated for each experiment in results. Then, 100μL/well of Cell Titer-Glo reagent was added and gently mixed for 15 minutes at room temperature (RT). |
Reaction Conditions | 0–200μM; 24h |
Applications | ICI 118,551 hydrochloride decreases viability in hemangioblastomas by inducing cell apoptosis. |
| Animal experiment [2]: | |
Animal models | 3xTg-alzheimer's disease (AD) mice |
Preparation Method | In these studies, only female 3xTg-AD mice were used. The selective ICI 118,551 hydrochloride was delivered via daily intraperitoneal (i.p.) injections for 6 weeks, at 1mg/kg. Control mice were injected with an equal volume of 0.9% NaCl. Mice were weighed immediately before, halfway throughout, and on the completion of the experiments |
Dosage form | 1mg/kg; ip; 45d |
Applications | ICI 118,551 hydrochloride exacerbates cognitive deficits in the AD mouse model. |
References: | |
| Cas No. | 72795-01-8 | SDF | |
| 别名 | ICI 118551 hydrochloride | ||
| 化学名 | (2R,3S)-1-[(7-methyl-2,3-dihydro-1H-inden-4-yl)oxy]-3-(propan-2-ylamino)butan-2-ol;hydrochloride | ||
| Canonical SMILES | CC1=C2CCCC2=C(C=C1)OCC(C(C)NC(C)C)O.Cl | ||
| 分子式 | C17H28ClNO2 | 分子量 | 313.86 |
| 溶解度 | DMF: 5 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 3 mg/ml,Ethanol: 2 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1861 mL | 15.9307 mL | 31.8613 mL |
| 5 mM | 0.6372 mL | 3.1861 mL | 6.3723 mL |
| 10 mM | 0.3186 mL | 1.5931 mL | 3.1861 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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