Dabuzalgron (previously codenamed R-450; Ro-115-1240) is a novel partial alphaA/IL receptor agonist that is administered in its hydrochloride form to control urethral smooth muscle contraction. The hemodynamic changes in the drug are very small and it is a potential drug for the treatment of stress urinary incontinence.
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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 HCl | ✔ | 98% | |||||||||||||||||
Cisatracurium besylate | ✔ | 96% | |||||||||||||||||
Yohimbine HCI | ✔ | 99+% | |||||||||||||||||
BMY 7378 |
++
α1D-adrenoceptor, pKi: 5.1 α2C-adrenoceptor, pKi: 6.54 |
+
β1-adrenoceptor, pIC50: 5.1 |
97% | ||||||||||||||||
Asenapine maleate |
++++
α2B-adrenergic receptor, pKi: 8.9 α2A-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 |
99% | |||||||||||||||||
Alfuzosin HCl | ✔ | 98% | |||||||||||||||||
Terazosin HCl | ✔ | 99% | |||||||||||||||||
Atipamezole | ✔ | 95% | |||||||||||||||||
Phentolamine methanesulfonate salt | ✔ | 99% | |||||||||||||||||
Doxazosin mesylate | ✔ | 99% | |||||||||||||||||
Tolazoline HCl | ✔ | 98% | |||||||||||||||||
Zenidolol HCl |
++++
β2-adrenergic receptor, Ki: 0.7nM β1-adrenergic receptor, Ki: 611nM |
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。 |
描述 | Dabuzalgron, also known as Ro 115-1240, is an orally active and selective agonist of the α-1A adrenergic receptor used for the treatment of urinary incontinence. Dabuzalgron prevents Doxorubicin-induced cardiotoxicity by protecting mitochondrial function. After 15 minutes of treatment, Dabuzalgron increased ERK phosphorylation in a dose-dependent manner with an EC50 value of 4.8 μM. ERK1/2 activation contributes to the cardioprotective effects of Dabuzalgron. At a concentration of 10 μM for 4 hours, Dabuzalgron protects NRVMs from Doxorubicin-induced cell death. Activation of α1A-AR by Dabuzalgron attenuates the deleterious effects of Doxorubicin on the mitochondrial membrane potential and attenuates the activation of factors important for the apoptotic response resulting from mitochondrial damage[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.15mL 0.63mL 0.31mL |
15.73mL 3.15mL 1.57mL |
31.47mL 6.29mL 3.15mL |
CAS号 | 219311-44-1 |
分子式 | C12H16ClN3O3S |
分子量 | 317.79 |
SMILES Code | CS(=O)(NC1=C(Cl)C=CC(OCC2=NCCN2)=C1C)=O |
MDL No. | MFCD13195546 |
别名 | Ro 115-1240 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, store in freezer, under -20°C |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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