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（ 母液浓度为 40 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们客服联系。| 中文名称: | Pirmenol hydrochloride 一键复制产品信息 | ||||
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| 英文名称: | Pirmenol hydrochloride | ||||
| 别名: | 盐酸吡美诺；盐酸吡哌醇 Cl-845;(±)-Pirmenolhydrochlorid | ||||
| CAS No: | 61477-94-9 | 分子式: | C22H31ClN2O | 分子量: | 374.95 |
| CAS No: | 61477-94-9 | ||||
| 分子式: | C22H31ClN2O | ||||
| 分子量: | 374.95 | ||||
包装规格：
5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：
溶于DMSO(≥28mg/ml)
产品描述：
基本信息
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产品编号： |
P11288 |
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产品名称： |
Pirmenol hydrochloride |
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CAS: |
61477-94-9 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃(氮气储存) |
6个月 |
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分子量： |
374.95 |
-20℃(氮气储存) |
1个月 |
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化学名： |
4-((2R,6S)-2,6-Dimethylpiperidin-1-yl)-1-phenyl-1-(pyridin-2-yl)butan-1-ol hydrochloride |
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Solubility (25°C)： |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.6670mL |
13.3351mL |
26.6702mL |
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5mM |
0.5334mL |
2.6670mL |
5.3340mL |
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10mM |
0.2667mL |
1.3335mL |
2.6670mL |
生物活性
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产品描述 |
Pirmenolhydrochloride通过阻断毒蕈碱性受体来抑制IK.ACh。 |
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靶点 |
0.1μM (IK.ACh) |
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体外研究 |
Pirmenol inhibits the carbachol-induced IK.ACh in a concentration-dependent manner.Pirmenol also inhibits the GTPγSinduced current although the concentrations of Pirmenol needed to inhibit the GTPγS-induced current are much higher than those to inhibit the carbachol-induced IK.ACh.The IC50 of Pirmenol for inhibition of the GTPγS-induced currents is 30μM.The inhibitory effect of Pirmenol on these IK.ACh is almost completely reversible and the outward current reappeared upon washout of Pirmenol.Pirmenol on the muscarinic acetylcholine receptor-operated K+current (IK.ACh) in atrial cells and on experimental atrial fibrillation in isolated guinea-pig hearts.In isolated atrial myocytes,Pirmenol concentration dependently inhibits the IK.ACh induced by carbachol or intracellular loading of GTPγS.In Langendorff-perfused hearts Pirmenol reverses the carbachol-induced decreases in effective refractory periods and atrial fibrillation threshold. |
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体内研究 |
The pyridine-methanol derivative Pirmenol hydrochloride is a new antiarrhythmic agent.Single-dose studies in rodents demonstrate a 10-to 15-fold difference between the po and iv LD50 values.In rats,the po LD50 is 359.9mg/kg and the iv LD50 is 23.6mg/kg.Mice LD50 values are 215.5 and 20.8mg/kg for po and iv routes,respectively.Short-term subacute iv toxicity studies in rats (2.5,5.0,and 7.5mg/kg) and dogs (2.5,5,and 10mg/kg) for 4 weeks elicite minimal reactions.Cardiac effects in dogs include drug related increases in heart rate,increases QRS duration,shortening of ST interval without evidence of cardiac tissue damage and mild local reaction at the injection site.Orally,Pirmenol is well tolerated for 13 weeks in rats receiving 25,50,and 100mg/kg/day while dogs given 5,10,and 15mg/kg/day shows anticholinergic effects at high levels (dryness of mucosae,body tremors).Heart rates are significantly accelerated only at the beginning of the study and QRS changes are seen with wide individual variations.No drug related tissue changes are elicited in these species.Teratology studies in rats (50,100,and 150mg/kg) and in rabbits (10,25,and 50mg/kg) show no overt effect on organogenesis but embryotoxicity is seen at 150mg/kg in rats. |
推荐实验方法(仅供参考)
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动物实验: |
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Mice and Rats The species and strains used in these studies are:male mice,21-29g;rats,116-261g;purebred beagle dogs,6.8-12.4kg;and rabbits,2.9kg average.For acute oral and intravenous studies and subacute oral studies,Pirmenol hydrochloride,hereafter referred to as Pirmenol,is supplied as bulk white crystalline compound of approximately 89% purity.Doses are calculated on the basis of base content.In acute studies,Pirmenol is given by gavage as 2 (mice) or 2.5% (rats) in aqueous solution;for iv administration,as 0.5 (mice) or 1% (rats) aqueous solution.In oral subacute studies in dogs,it is given in gelatin capsules,and in rats,it is mixed with the diet to yield the intended dose concentrations.Rabbits received the drug in a 5% aqueous solution by intragastric intubation.For subacute iv studies,Pirmenol is supplied in sterile vials as a 1% solution.In rats,iv injection approximated 0.6mL/min,and in dogs,the drug is administered via an infusion pump at the rate of 1mg/kg/min. |
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保存条件：
-20℃
UN码：
HazardClass：
危害声明：
安全说明：
搜索质检报告(COA)
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
(2).jpg)
体内配方的制备方法: 取 50μLDMSO 母液，添加 300 μLPEG300 混匀澄清，再加 50μLTween80, 混匀澄清，再加 600μLSaline/PBS/ddH2O 混匀澄清
方案所需的各种助溶剂如： DMSO ， PEG300 / PEG400 ， Tween 80 ， SBE-β-CD ， 玉米油 等， 均可点击跳转或在网站搜索购买。
母液，添加 300 μLPEG300 混匀澄清，再加 50μLTween80, 混匀澄清，再加 600μLSaline/PBS/ddH2O 混匀澄清方案所需的各种助溶剂如： DMSO ， PEG300 / PEG400 ， Tween 80 ， SBE-β-CD ， 玉米油 等， 均可点击跳转或在网站搜索购买。
以上为“动物实验计算换算器”的使用方法举例，并不是具体某个试剂的配制，请根据您的实验动物和给药方式选择适当的溶解方案。
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/PBS/ddH2O，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。
剂量转换
对于不同动物的给药剂量换算，您也可以参考 更多
