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Rilmenidine phosphate {[allProObj[0].p_purity_real_show]}

货号:A866594

Rilmenidine Phosphate is an oxazole-derived agonist of adrenergic receptor α2 and Imidazoline receptor, used in trials studying the treatment of hypertension and chronic kidney disease.

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Rilmenidine phosphate 化学结构 CAS号:85409-38-7
Rilmenidine phosphate 化学结构
CAS号:85409-38-7
Rilmenidine phosphate 3D分子结构
CAS号:85409-38-7
Rilmenidine phosphate 化学结构 CAS号:85409-38-7
Rilmenidine phosphate 3D分子结构 CAS号:85409-38-7
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Rilmenidine phosphate 纯度/质量文件 产品仅供科研

货号:A866594 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 α2A, pKi: 7.1

adrenoceptor α2C, pKi: 7.2

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 ++++

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。
产品名称 Autophagy 其他靶点 纯度
SBI-0206965 +++

ULK2, IC50: 711 nM

ULK1, IC50: 108 nM

97%
Hydroxychloroquine sulfate 99%
Valproic acid sodium HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

99%+
MRT68921 hydrochloride ++++

ULK2, IC50: 1.1 nM

ULK1, IC50: 2.9 nM

99%+
ROC-325 99%+
Autophinib +++

Autophagy, IC50: 40 nM

97%
Lys05 99%+
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。

Rilmenidine phosphate 生物活性

描述 α2-Adrenoceptors (α2-AR) found in the cardiomyocyte's sarcolemma represent a very important negative feedback for control of myocardial contractility by endogenous catecholamines[2]. Rilmenidine is a clinically approved anti-hypertensive agent that acts by activating ADRA2/α2-adrenoceptors and imidazoline-1 receptors (I1Rs) in the brain and periphery. It can be a mTOR-independent autophagy inducers. Stable inducible PC12 cells expressing either wild-type (23Q) or expanded polyglutamine (74Q) huntingtin both showed a significant increase in LC3-II (microtubule-associated protein 1 light chain) when treated with rilmenidine for 24 h[3]. Sinus rate, corrected sinus recovery time (CSRT) and Wenckebach point (WP) were measured in seven intact dogs. Atrial rate and atrial effective refractory period (AERP) were measured in six atrioventricular (AV)-blocked dogs with ventricular pacing. Each dog received with at least a three-day interval rilmenidine as dihydrogen phosphate in four successive intravenous injections, 30 min apart. In intact dogs, rilmenidine was administered at 50, 50, 100 and 200 μg/kg. In AV-blocked dogs, doses of rilmenidine were 25, 25, 50 and 100 μg/kg. Rilmenidine decreased sinus rate and atrial rate from the first dose. A lengthening of CSRT and a lowering of WP were observed at all doses with rilmenidine. A shortening of AERP was also seen with rilmenidine from the second dose[4].

Rilmenidine phosphate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02539810 Hypertension ... 展开 >>Hypertension Resistant to Conventional Therapy Angiographically Proven Grade III Unilateral or Bilateral Atherosclerotic Renal Artery Stenosis (ARAS) Greater Than or Equal to 60 Percent 收起 << Phase 4 Terminated - France ... 展开 >> Hopital Pasteur Nice, Alpes-Maritimes, France, 06002 Hopital Saint Andre - CHU Bordeaux Bordeaux, Gironde, France, 33075 Hopital Rangueil - CHU Toulouse Toulouse, Haute-Garonne, France, 31059 Hopital Lapeyronie - CHU Montpellier Montpellier, Herault, France, 34295 Hopital Arthur Gardiner Dinard, Ille-et-Vilaine, France, 35800 Hopital Pontchaillou - CHU Rennes Rennes, Ille-et-Vilaine, France, 35033 Groupe Hospitalier Mutualiste Grenoble, Isere, France, 38028 Hopital Michallon - CHU Grenoble La Tronche, Isere, France, 38700 Institut Lorrain du Cœur et des Vaisseaux Louis Mathieu Vandoeuvre les Nancy, Meurthe-et-Moselle, France, 54500 Hopital de Brabois Vandoeuvre les Nancy, Meurthe-et-Moselle, France, 54511 Hopital Cardiologique - CHRU Lille Lille, Nord, France, 59037 CHU Clermont-Ferrand Clermont-Ferrand, Puy-de-Dome, France, 63000 Hopital de la Croix-Rousse - CHU Lyon Lyon, Rhone, France, 69004 Hopital de la Pitie Salpetriere Paris, France, 75013 Hopital Europeen Georges Pompidou (HEGP) Paris, France, 75015 收起 <<
NCT00892892 Chronic Kidney Disease ... 展开 >> Hypertension 收起 << Phase 4 Withdrawn - Germany ... 展开 >> University of Erlangen-Nuremberg, CRC, med. Clinic 4 Erlangen, Bavaria, Germany, 91054 收起 <<

Rilmenidine phosphate 参考文献

[1]Tonet J, Guillet C, et al. Electrophysiological effects of intravenous rilmenidine in man. Eur J Clin Pharmacol. 1991;41(6):537-40.

[2]Maltsev AV, Evdokimovskii EV, Kokoz YM. α2-Adrenoceptor signaling in cardiomyocytes of spontaneously hypertensive rats starts to impair already at early age. Biochem Biophys Res Commun. 2019;512(4):908-913.

[3]Rose C, Menzies FM, Renna M, et al. Rilmenidine attenuates toxicity of polyglutamine expansions in a mouse model of Huntington's disease. Hum Mol Genet. 2010;19(11):2144-2153.

[4]Boucher M, Dubar M, Chassaing C, Vivet P, Duchêne-Marullaz P. Cardiac electrophysiological effects of rilmenidine, a novel antihypertensive agent, in the conscious dog: comparison with clonidine. Life Sci. 1994;54(22):PL381-PL387.

Rilmenidine phosphate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.59mL

0.72mL

0.36mL

17.97mL

3.59mL

1.80mL

35.94mL

7.19mL

3.59mL

Rilmenidine phosphate 技术信息

CAS号85409-38-7
分子式C10H19N2O5P
分子量 278.24
别名
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: 4 mg/mL(14.38 mM),配合低频超声,并水浴加热至45℃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: 85 mg/mL(305.49 mM),配合低频超声助溶

动物实验配方
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