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Anisotropine Methylbromide

Anisotropine Methylbromide

产品编号 T4981   CAS 80-50-2

Anisotropine Methylbromide 是一种抗胆碱能药物,已用于缓解胃肠道痉挛和抑制胃酸分泌。

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Anisotropine Methylbromide Chemical Structure
Anisotropine Methylbromide, CAS 80-50-2
规格 价格/CNY 货期 数量
5 mg ¥ 248 现货
10 mg ¥ 420 现货
25 mg ¥ 630 现货
50 mg ¥ 940 现货
100 mg ¥ 1,200 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: Anisotropine Methylbromide (T4981)
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纯度: 99.73%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Anisotropine Methylbromide is an anticholinergic agent and has been used for relief of gastrointestinal spasm and for the suppression of gastric acid secretion.
靶点活性 EP3:68.9 nM (EC50), EP2:6.2 nM (EC50), DP1:0.6 nM (EC50), IP:1.9 nM (EC50)
体外活性 Treprostinil has a high affinity for the IP, EP2 and DP1 receptors (Ki: 32, 3.6 and 4.4 nM, respectively), low affinity for EP1 and EP4 receptors and even lower affinity for EP3, FP, and TP receptors. Activation of IP, DP1 and EP2 receptors can all result in vasodilatation of human pulmonary arteries[1]. Treprostinil inhibits the viability of cultured endothelial colony forming cells. Endothelial colony forming cells proliferation is stimulated by conditioned media from Treprostinil pretreated mesenchymal stem cells [2].
体内活性 Treprostinil is most efficacious in raising intracellular cAMP levels in murine and human hematopoietic stem and progenitor cells [2]. Treprostinil preserves the sinusoidal endothelial cell lining and reduces platelet deposition early post-transplantation compared to placebo. Hepatic tissue blood flow is significantly compromised in the placebo group, whereas treprostinil maintains blood flow similar to normal levels [3]. Treprostinil treatment significantly increases the vessel-forming ability of endothelial colony forming cells combined with mesenchymal stem cells in Matrigel implanted in nude mice. Silencing VEGF-A gene in mesenchymal stem cells also blocks the pro-angiogenic effect of Treprostinil [4]. Treatment with Treprostinil significantly reduces the recruitment of cells compared to normoxic mice. Treprostinil also reduces right ventricular systolic pressure and slightly reduces the vascular remodeling but fails to reverse the right ventricular hypertrophy [5].
细胞实验 Human or murine hematopoietic stem and progenitor cells are incubated in the presence of vehicle or the combination of 10 μM Treprostinil and 30 μM forskolin at 37°C for 1 hour and 24 hours. After washing with phosphate-buffered saline at 4°C, cells are stained for externalized phosphatidylserine with the apoptosis kit [2].
动物实验 Male Lewis rats weighing 200-300 g are used in the study. Donor animals receive treprostinil or placebo 24 h before hepatectomy and the corresponding recipient animal receive a similar treatment until the time of sacrifice. The surgeon is blinded to treatment. Recipients are sacrificed at 1, 3, 6, 24 and 48 h post-transplantation to examine the early events after IRI. Treprostinil (100 ng/kg/min) or placebo is administered subcutaneously via an Alzet implantable osmotic pump. This dose is selected to achieve a steady-state plasma concentration in the range of 5-20 ng/mL [3]. . Bone marrow transplanted (BMT) mice are divided into five different groups with each group consisting of 6 to 10 mice. One group of mice is exposed to hypoxia (10% inspired oxygen fraction) in a normobaric chamber whereas the second group (control BMT) of animals are placed in a normoxic chamber with a normal oxygen environment (21% inspired O2 fraction) for 28 days. Sham group mice receive saline treatment whereas two other groups of mice receive Treprostinil infusions of different dose levels (14 ng/kg and 70 ng/kg per minute) and are exposed to hypoxia for 4 weeks. For comparison, human infusion rates in PAH therapy vary from 10 to 60 ng/kg per min[5].
分子量 362.35
分子式 C17H32BrNO2
CAS No. 80-50-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (137.99 mM)

H2O: 198.7 mM

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.7598 mL 13.7988 mL 27.5976 mL 68.9941 mL
5 mM 0.552 mL 2.7598 mL 5.5195 mL 13.7988 mL
10 mM 0.276 mL 1.3799 mL 2.7598 mL 6.8994 mL
20 mM 0.138 mL 0.6899 mL 1.3799 mL 3.4497 mL
50 mM 0.0552 mL 0.276 mL 0.552 mL 1.3799 mL
100 mM 0.0276 mL 0.138 mL 0.276 mL 0.6899 mL

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TargetMol Library Books参考文献

1. Freston JW, et al. A double-blind evaluation of the nocturnal antisecretory effects of anisotropine methylbromide in man. Dose response and duration of action studies. J Clin Pharmacol. 1977 Jan;17(1):29-36.
Treprostinil diethanolamine Pirmagrel Darbufelone Neoechinulin A Ozagrel hydrochloride Treprostinil Sodium Latifolin AH 6809

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌上市药物库 GPCR靶点分子库 抑制剂库 药物功能重定位化合物库 膜蛋白靶向化合物库 经典已知活性库 非甾体类抗炎化合物库 神经信号分子库 NO PAINS 化合物库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (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,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

Anisotropine Methylbromide 80-50-2 GPCR/G Protein Immunology/Inflammation Neuroscience Prostaglandin Receptor AChR gastric acid mAChR Muscarinic acetylcholine receptor Inhibitor inhibit anticholinergic Octatropine peptic ulcers Anisotropine muscarinic inhibitor

 

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