2. GPCR/G Protein Neuronal Signaling Apoptosis Metabolic Enzyme/Protease
  3. Adrenergic Receptor Caspase Apoptosis Aldose Reductase Neurokinin Receptor
  4. Esmolol

Esmolol 是一种超短效心脏选择性 β1-肾上腺素 (β1-adrenergic) 能阻滞剂。Esmolol 通过激活 NK1 受体 (Neurokinin 1 Receptor)，发挥其抗心律失常作用。Esmolol 减轻复苏后心肌功能障碍。Esmolol 通过抑制醛糖还原酶 (aldose reductase)、晚期糖基化终产物的产生和促进成纤维细胞的迁移改善糖尿病的伤口愈合。Esmolol 可用于研究心律失常等心脏疾病以及糖尿病足溃疡。

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Esmolol

Esmolol Chemical Structure

CAS No. : 81147-92-4

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Esmolol 的其他形式现货产品:

Other Forms of Esmolol:

Esmolol 相关抗体

Top Publications Citing Use of Products

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α adrenergic receptor β adrenergic receptor

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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NK1R NK2R NK3R

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Esmolol is an ultra-short-acting cardioselective β1-adrenergic blocker. Esmolol exerts its antiarrhythmic effect by activating Neurokinin 1 Receptor. Esmolol attenuates post resuscitation myocardial dysfunction. Esmolol improves diabetic wound healing by inhibiting aldose reductase and the production of advanced glycation end products and promoting fibroblast migration. Esmolol can be used to study cardiac diseases such as arrhythmias and diabetic foot ulcers[1][2][3].

IC50 & Target[1][2][3]

β adrenergic receptor

 

Caspase 3

 

体外研究
(In Vitro)

Esmolol hydrochloride (0-1 mM) 可抑制醛糖还原酶活性，IC50 估计值为 150 µM，并可抑制红细胞中 59% 的山梨醇形成[1]。
Esmolol hydrochloride (0.5-1 mM，10 分钟) 可抑制晚期糖基化终产物 (AGEs) 的形成[1]。
Esmolol hydrochloride (0.01-1000 µM，8-48 小时) 可促进 HFF-1、Ea.hy926 和 HaCaT 细胞的迁移能力，且无细胞毒性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Esmolol 相关抗体:

Cell Migration Assay [1]

Cell Line: HFF-1, Ea.hy926, HaCaT cells
Concentration: 0.01 μM, 0.1 μM, 1 μM, 10 μM, 50 μM, 100 μM, 500 μM, 100 μM
Incubation Time: 8 h, 14 h, 16 h, 22 h, 24 h, 42 h, 48 h
Result: Promoted the ability to migrate, with low migration at 100 and 500 µM.
体内研究
(In Vivo)

Esmolol hydrochloride (7%-20%，局部应用，每日两次) 可改善 Streptozotocin (HY-13753) 诱发的糖尿病无毛大鼠的 NO 诱导、胶原周转和羟脯氨酸水平，并改善其重塑和伤口愈合[1]。
Esmolol (10 mg/kg，0.3 mL，静脉注射，一次) 在永久性冠状动脉闭塞 (CAO) 大鼠模型中，通过上调 NK1 受体表现出抗心律失常作用[2]。
Esmolol (300 μg/kg，肾上腺素20 μg/kg，静脉注射，一次) 在近交系五指山小型猪中通过减少凋亡来保护心肌组织，改善复苏后心肌功能障碍[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Streptozotocin-induced (35 mg/kg/day for 5 consecutive days) diabetic hairless rats model[1]
Dosage: 7, 14, and 20%
Administration: topical applied, twice daily
Result: Increased the total nitrite content and NO level in wound tissue by 44% and 112% in the G14 group compared with the diabetic control group and the vehicle control group, and by 8% and 59% in the G20 group compared with the diabetic control group and the vehicle control group.
Improved collagen content, hydroxyproline levels, increased hydroxyproline levels by 22% and 44% in the G14 group, and 21% and 43% in the G20 on day 7; increased hydroxyproline levels by 6% and 13% in the G14 group, increased hydroxyproline levels by 41% and 49% in the G20 group on day 14, compared with the diabetic control and vehicle control groups.
Improved healing in G20 group and closer to normal intact diabetic skin (wounds were not completely closed on day 19) .
Animal Model: CAO Male Sprague-Dawley rats (weighing 260 g-280 g) model[2]
Dosage: 10 mg/kg, in 0.3 mL
Administration: i.v., once
Result: Reduced ventricular ectopic beat (VEB) by 66%, and reduced the incidence, number, and duration of VT and VF by 66%, 92%, and 95%, respectively .
Attenuated the arrhythmogenic effects of D-SP, reducing the VEB by 45%, the morbidity rate, the episodes and the durations of VT & VF by 86%, 62% and 50% respectively, in 9-23 min following the coronary artery occlusion (CAO) (14 min-28 min after the injection of esmolol).
Increased NK1-R mRNA and protein, by 72% and 19% respectively, at 15 min after the CAO.
Animal Model: Inbred Wuzhishan miniature pigs (12-14 months of age, 30 kg) model[3]
Dosage: 300 μg/kg with Epinephrine (HY-B0447B) 20 μg/kg
Administration: i.v., once
Result: Reduced the number of shocks, defibrillation energy, return of spontaneous circulation (ROSC) time and 4 h heart rate (HR), and increased the 24 h survival rate, 4-6 h CO values, 4 h mean aortic pressure (MAP) value, and 4 h left ventricular dp/dtmax.
Reduced serum cTnI, lactate concentrations and , myocardial malondialdehyde (MDA) content, increased ATPase and SOD levels.
Reduced caspase-3 proteolytic activation, mRNA levels, and TUNEL-positive cells, and attenuated apoptotic effects by upregulating Bcl-2/Bax protein levels.
Clinical Trial
分子量

295.37

Formula

C16H25NO4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Esmolol 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Esmolol81147-92-4Adrenergic ReceptorCaspaseApoptosisAldose ReductaseNeurokinin ReceptorBeta ReceptorNK receptorTachykinin receptorBlockerArrhythmiasDiabetic foot ulcersfibroblastsInhibitorinhibitorinhibit

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