Gadobutrol
(Synonyms: 钆布醇; ZK 135079) 目录号 : GC36098
Gadobutrol (Gadovist, Gadavist,ZK 135079) is a non-ionic macrocyclic gadolinium-based contrast agent (GBCA) that is usedfor tissue contrast enhancement in magnetic resonance imaging (MRI).
Cas No.:770691-21-9;138071-82-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Gadobutrol (Gadovist, Gadavist,ZK 135079) is a non-ionic macrocyclic gadolinium-based contrast agent (GBCA) that is usedfor tissue contrast enhancement in magnetic resonance imaging (MRI).
[1] Lesley J Scott. Clin Drug Investig. 2018 Aug;38(8):773-784.
| Cas No. | 770691-21-9;138071-82-6 | SDF | |
| 别名 | 钆布醇; ZK 135079 | ||
| Canonical SMILES | OCC1[N]2(CC[N]3(C4)CC[N]5(C6)CC[N]7(C8)CC2)[Gd+3]357([O-]C4=O)([O-]C8=O)([O-]C6=O)O([H])C1CO | ||
| 分子式 | C18H31GdN4O9 | 分子量 | 604.71 |
| 溶解度 | Water: 20 mg/mL (33.07 mM) | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6537 mL | 8.2684 mL | 16.5369 mL |
| 5 mM | 0.3307 mL | 1.6537 mL | 3.3074 mL |
| 10 mM | 0.1654 mL | 0.8268 mL | 1.6537 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Gadobutrol: A Review in Contrast-Enhanced MRI and MRA
Clin Drug Investig 2018 Aug;38(8):773-784.PMID:30006819DOI:10.1007/s40261-018-0674-9.
Intravenous Gadobutrol [Gadovist™ (EU); Gadavist® (USA)] is a second-generation, extracellular non-ionic macrocyclic gadolinium-based contrast agent (GBCA) that is approved for use in paediatric (including term neonates) and adult patients undergoing diagnostic contrast-enhanced (CE) MRI for visualization of pathological lesions in all body regions or for CE MRA to evaluate perfusion and flow-related abnormalities. Its unique physicochemical profile, including its high thermostability and proton relaxation times, means that Gadobutrol is formulated at twice the gadolinium ion concentration of other GBCAs, resulting in a narrower bolus and consequently, improved dynamic image enhancement. Based on > 20 years of experience in the clinical trial and real-world settings (> 50 million doses) and its low risk for developing nephrogenic systemic fibrosis (NSF), Gadobutrol represents an effective and safe diagnostic GBCA for use in CE MRI and MRA to visualize pathological lesions and vascular perfusion and flow-related abnormalities in all body regions in a broad spectrum of patients, including term neonates and other paediatric patients, young and elderly adult patients, and those with moderate or severe renal or hepatic impairment or cardiovascular (CV) disease.
Gadobutrol: a review of its use for contrast-enhanced magnetic resonance imaging in adults and children
Clin Drug Investig 2013 Apr;33(4):303-14.PMID:23435930DOI:10.1007/s40261-013-0066-0.
Since the introduction of the first gadolinium-based contrast agent (GBCA) approximately 25 years ago, magnetic resonance imaging (MRI) using GBCAs has revolutionized diagnostic and follow-up imaging of pathological lesions, with clinical applications expanded to encompass almost all fields of medicine. Intravenous Gadobutrol (Gadovist™ [EU]; Gadavist(®) [USA]) is a second-generation extracellular non-ionic macrocyclic GBCA that is used in patients undergoing diagnostic contrast-enhanced MRI for visualization of pathological lesions in the CNS and all other body regions or for contrast-enhanced magnetic resonance angiography (MRA) to evaluate perfusion and flow-related abnormalities. Its unique physicochemical profile, along with the high thermostability of macrocyclic GBCAs, means Gadobutrol is formulated at twice the gadolinium ion concentration of other currently licensed GBCAs. This reduces the injection volume and provides a narrower bolus, thereby improving image enhancement. Based on extensive clinical experience in a broad range of patients, including paediatric and adult patients (younger and elderly adults), and those with moderate to severe hepatic or renal impairment or cardiovascular disorders, Gadobutrol is an effective and generally well tolerated extracellular GBCA for patients undergoing diagnostic contrast-enhanced MRI and contrast-enhanced MRA. As with all macrocyclic GBCAs, the potential for Gadobutrol to cause nephrogenic systemic fibrosis appears to be lower than with linear GBCAs.
Gadobutrol enhances T1-weighted MRI of nerve cells
Toxicol Lett 2019 Jun 15;308:17-23.PMID:30902667DOI:10.1016/j.toxlet.2019.03.005.
Three-dimensional T1-weighted MRI of mouse brain in vivo (9.4 T, 80 μm isotropic resolution) identified assemblies of nerve cell bodies in the habenula, hippocampal formation, locus coeruleus, dorsal motor nucleus of vagus, and nucleus ambiguus as high signal intensities, while suppressing the signals of white matter by magnetization transfer and of extracellular water protons by saturation. These observations indicate the presence of intracellular water protons with T1 values shortened by paramagnetic ions as the source of the bright signal. One day after an intraventricular injection of Gadobutrol, a macrocyclic gadolinium-based contrast agent, T1-weighted MRI signal intensities of the nerve cell assemblies in the habenula, hippocampal formation, and locus coeruleus increased significantly. With simultaneous saturation of long-T1 protons of extracellular water, this finding indicates a T1-shortening of the intracellular water protons as a result of their interaction with gadolinium ions.
Simultaneous [18F]fluoride and Gadobutrol enhanced coronary positron emission tomography/magnetic resonance imaging for in vivo plaque characterization
Eur Heart J Cardiovasc Imaging 2022 Sep 10;23(10):1391-1398.PMID:35015852DOI:10.1093/ehjci/jeab276.
Aims: 18F-sodium fluoride ([18F]fluoride) and Gadobutrol are promising probes for positron emission tomography (PET) and magnetic resonance imaging (MRI) characterizing coronary artery disease (CAD) activity. Unlike [18F]fluoride-PET/computed tomography (CT), the potential of PET/MR using [18F]fluoride and Gadobutrol simultaneously, has so far not been evaluated. This study assessed feasibility and diagnostic potential of [18F]fluoride and Gadobutrol enhanced dual-probe PET/MR in patients with CAD. Methods and results: Twenty-one patients (age, 66.7 ± 6.7 years) with CAD scheduled for invasive coronary angiography (XCA) underwent simultaneous [18F]fluoride (mean activity/effective dose: 157.2 ± 29.7 MBq/3.77 ± 0.72 mSv) and Gadobutrol enhanced PET/MR on an integrated PET/MRI (3 T) scanner. Optical coherence tomography (OCT) was used as reference. Target-to-background ratio (TBR, [18F]fluoride-PET) and contrast-to-noise ratio (CNR) values (MRI, Gadobutrol) were calculated for each coronary segment. Previously suggested PET/CT-TBR thresholds for adverse coronary events were evaluated. High-risk plaques, i.e. calcified and non-calcified thin-cap fibroatheromas (TCFAs) were predominantly located in segments with a TBR >1.28 (P = 0.012). Plaques containing a lipid core on OCT, were more frequently detected in segments with a TBR >1.25 (P < 0.001). TBR values significantly correlated with maximum calcification thickness (P = 0.009), while fibrous cap thickness was significantly less in segments with a TBR >1.28 (P = 0.044). Above a TBR threshold of >1.28, CNR values significantly correlated with the presence of calcified TCFAs (P = 0.032). Conclusion: Simultaneous [18F]fluoride and Gadobutrol dual-probe PET/MRI is feasible in clinical practice and may facilitate the identification of high-risk patients. The combination of coronary MR-derived CNR values post Gadobutrol and [18F]fluoride based TBR values may improve identification of high-risk plaque features.
Gadobutrol-Enhanced Cardiac Magnetic Resonance Imaging for Detection of Coronary Artery Disease
J Am Coll Cardiol 2020 Sep 29;76(13):1536-1547.PMID:32972530DOI:10.1016/j.jacc.2020.07.060.
Background: Gadolinium-based contrast agents were not approved in the United States for detecting coronary artery disease (CAD) prior to the current studies. Objectives: The purpose of this study was to determine the sensitivity and specificity of Gadobutrol for detection of CAD by assessing myocardial perfusion and late gadolinium enhancement (LGE) imaging. Methods: Two international, single-vendor, phase 3 clinical trials of near identical design, "GadaCAD1" and "GadaCAD2," were performed. Cardiovascular magnetic resonance (CMR) included gadobutrol-enhanced first-pass vasodilator stress and rest perfusion followed by LGE imaging. CAD was defined by quantitative coronary angiography (QCA) but computed tomography coronary angiography could exclude significant CAD. Results: Because the design and results for GadaCAD1 (n = 376) and GadaCAD2 (n = 388) were very similar, results were summarized as a fixed-effect meta-analysis (n = 764). The prevalence of CAD was 27.8% defined by a ≥70% QCA stenosis. For detection of a ≥70% QCA stenosis, the sensitivity of CMR was 78.9%, specificity was 86.8%, and area under the curve was 0.871. The sensitivity and specificity for multivessel CAD was 87.4% and 73.0%. For detection of a 50% QCA stenosis, sensitivity was 64.6% and specificity was 86.6%. The optimal threshold for detecting CAD was a ≥67% QCA stenosis in GadaCAD1 and ≥63% QCA stenosis in GadaCAD2. Conclusions: Vasodilator stress and rest myocardial perfusion CMR and LGE imaging had high diagnostic accuracy for CAD in 2 phase 3 clinical trials. These findings supported the U.S. Food and Drug Administration approval of gadobutrol-enhanced CMR (0.1 mmol/kg) to assess myocardial perfusion and LGE in adult patients with known or suspected CAD.