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

货号：A866594 Ambeed 开学季，买赠积分，赢豪礼

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]}
批次查询： 批次纯度:

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产品名称 Adrenergic Receptor ↓ α-adrenergic receptor ↓ β-adrenergic receptor ↓ 其他靶点 纯度
Ivabradine HCl ✔ {[allProObj[0].p_purity_real_show]}
Maprotiline hydrochloride ✔ {[allProObj[0].p_purity_real_show]}
Cisatracurium besylate ✔ {[allProObj[0].p_purity_real_show]}
Yohimbine HCI ✔ {[allProObj[0].p_purity_real_show]}
BMY 7378 ++

α1D-adrenoceptor, pKi: 5.1

α2C-adrenoceptor, pKi: 6.54

 		+

β1-adrenoceptor, pIC50: 5.1

 		{[allProObj[0].p_purity_real_show]}
Asenapine maleate ++++

α2B-adrenergic receptor, pKi: 8.9

α2A-adrenergic receptor, pKi: 8.9

 		{[allProObj[0].p_purity_real_show]}
Piribedil ++

adrenoceptor α2A, pKi: 7.1

adrenoceptor α2C, pKi: 7.2

 		{[allProObj[0].p_purity_real_show]}
Prazosin HCl ✔ {[allProObj[0].p_purity_real_show]}
Silodosin ✔ {[allProObj[0].p_purity_real_show]}
Phenoxybenzamine HCl ✔ {[allProObj[0].p_purity_real_show]}
Naftopidil +++

α1D-adrenergic receptor, Ki: 20 nM

α1A-adrenergic receptor, Ki: 3.7 nM

 		{[allProObj[0].p_purity_real_show]}
Naftopidil 2HCl +

α1-adrenergic receptor, IC50: 0.2 μM

 		{[allProObj[0].p_purity_real_show]}
Alfuzosin HCl ✔ {[allProObj[0].p_purity_real_show]}
Terazosin HCl ✔ {[allProObj[0].p_purity_real_show]}
Atipamezole ✔ {[allProObj[0].p_purity_real_show]}
Phentolamine methanesulfonate salt ✔ {[allProObj[0].p_purity_real_show]}
Doxazosin mesylate ✔ {[allProObj[0].p_purity_real_show]}
Tolazoline HCl ✔ {[allProObj[0].p_purity_real_show]}
Zenidolol hydrochloride ++++

β2-adrenergic receptor, Ki: 0.7nM

β1-adrenergic receptor, Ki: 611nM

 		{[allProObj[0].p_purity_real_show]}
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

 		{[allProObj[0].p_purity_real_show]}
Hydroxychloroquine sulfate ✔ {[allProObj[0].p_purity_real_show]}
Valproic acid sodium ✔ HDAC {[allProObj[0].p_purity_real_show]}
PFK-015 ++

PFKFB3, IC50: 207 nM

 		{[allProObj[0].p_purity_real_show]}
MRT68921 hydrochloride ++++

ULK2, IC50: 1.1 nM

ULK1, IC50: 2.9 nM

 		{[allProObj[0].p_purity_real_show]}
ROC-325 ✔ {[allProObj[0].p_purity_real_show]}
Autophinib +++

Autophagy, IC50: 40 nM

 		{[allProObj[0].p_purity_real_show]}
Lys05 ✔ {[allProObj[0].p_purity_real_show]}
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

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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

Tags: Rilmenidine | 85409-38-7 | Imidazoline Receptor | I1 Imidazoline Receptor/α2-Adrenoceptor Agonist | Neuronal Signaling | GPCR/G Protein | Apoptosis | Autophagy | Imidazoline Receptor | Adrenergic Receptor | Apoptosis | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Rilmenidine phosphate 纯度/质量文件 | Rilmenidine phosphate 亚型比较 | Rilmenidine phosphate 生物活性 | Rilmenidine phosphate 临床数据 | Rilmenidine phosphate 参考文献 | Rilmenidine phosphate 实验方案 | Rilmenidine phosphate 技术信息

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