4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine
目录号 : GC30952
4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine是一种有效的淀粉样蛋白显像剂，其与淀粉样蛋白Amyloid-β(1-40)结合的KD值为1.7nM。
Cas No.:566169-98-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Mice[1]Studies are performed in female Swiss-Webster mice (23-35 g). The mice are injected in a lateral tail vein with 0.37-3.7 MBq (10-100 µCi) of a high specific activity (>7.4 GBq/µmol) 11C-4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine contained in <0.10 mL of a solution of 93% isotonic saline and 7% ethanol. The mice are anesthetized and killed by cardiac excision following cardiac puncture to obtain arterial blood samples at 2 or 30 min postinjection. The mouse brains are rapidly excised and divided into cerebellum and remaining whole brain (including brain stem) fractions. The brain samples are counted in a gamma wellcounter, and the counts are decay-corrected to the time of injection relative to 11C standards prepared from the injection solution to determine the percent injected dose (%ID) in the samples. The brain samples are weighed to determine the percent injected dose per gram tissue (%ID/g), and this quantity is multiplied by the whole body weight (in kg) to determine the body-weight normalized radioactivity concentration [(%ID-kg)/g] of each tissue sample[1]. |
References: [1]. Mathis CA, et al. Synthesis and evaluation of 11C-labeled 6-substituted 2-arylbenzothiazoles as amyloid imaging agents. J Med Chem. 2003 Jun 19;46(13):2740-54. | |
4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine is a potent amyloid imaging agent which binds to Amyloid-β (1-40) with a KD of 1.7 nM.
Alzhermer's Disease (AD) is a neurodegenerative illness characterized by memory loss and other cognitive deficits. The ability to quantify amyloid load before treatment is critical to the efficient development of this class of drugs[2]. Brain entry in control mice and baboons is high for 4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine. Staining of AD frontal cortex tissue sections with 4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine indicates the selective binding of the compound to amyloid plaques and cerebrovascular amyloid. The encouraging properties of the compound support the choice of this derivative for further evaluation in human subject studies of brain Amyloid-βdeposition. The brain radioactivity concentrations (%ID-kg/g) of 4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine is remarkably similar in mice and baboons (0.21 vs 0.27). The rate of clearance of radioactivity is considerably slower from baboon brain than from mouse brain, although the rank order of clearance rate is similar in mice and baboons. The tissue staining findings utilizing nonradiolabeled, fluorescent 4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine are similar to those reported for BTA-1. Both amyloid plaques and cerebrovascular amyloid are stained by 4-(6-Bromo-2-benzothiazolyl)-N-methylbenzenamine in a manner similar to serial sections stained with an antibody to Amyloid-β, and relatively little tissue background staining is observed[1].
[1]. Mathis CA, et al. Synthesis and evaluation of 11C-labeled 6-substituted 2-arylbenzothiazoles as amyloid imaging agents. J Med Chem. 2003 Jun 19;46(13):2740-54. [2]. Klunk W, et al. Amyloid imaging as a surrogate marker for efficacy of anti-amyloid therapies.
| Cas No. | 566169-98-0 | SDF | |
| Canonical SMILES | CNC1=CC=C(C2=NC3=CC=C(Br)C=C3S2)C=C1 | ||
| 分子式 | C14H11BrN2S | 分子量 | 319.22 |
| 溶解度 | Soluble in DMSO | 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 | 3.1326 mL | 15.6632 mL | 31.3264 mL |
| 5 mM | 0.6265 mL | 3.1326 mL | 6.2653 mL |
| 10 mM | 0.3133 mL | 1.5663 mL | 3.1326 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 |
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| % 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。
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( E)-4-(2-(6-(2-(2-(2-([18F]-fluoroethoxy)ethoxy)ethoxy)pyridin-3-yl)vinyl)- N-methylbenzenamine
Alzheimer's disease (AD) is a form of dementia with a gradual memory loss and a progressive decline in mental functions overtime (1, 2). It is characterized pathologically by neuronal loss, extracellular senile plaques (aggregates of amyloid-beta peptides consisting of 40 to 42 amino acids) and intracellular neurofibrillary tangles (filaments of microtubule-binding hyper-phosphorylated protein tau) in the brain, especially in the hippocampus and associative regions of the cortex (3, 4). 汕-amyloid peptides and tau protein are implicated as the main causes of neuronal degeneration and cell death (5, 6).
Early diagnosis of AD is important for treatment consideration and disease management (7). Various 汕-amyloid imaging agents have been developed for magnetic resonance imaging (MRI), single photon emission computed tomography (SPECT), and positron emission tomography (PET) (8-13). The binding of different derivatives of Congo red, thioflavin, stibene, and aminonaphthalene has been studied in human post-mortem brain tissue and in transgenic mice. Out of these analogues, 2-(1-(6-[(2-[18F]fluoroethyl)(methyl)amino]-2-naphthyl)ethylidene)malono nitrile ([18F]FDDNP) was studied in humans, showing more binding in the brains of patients with AD than in those of healthy people (14). However, [18F]FDDNP showed low signal-to-noise ratios for PET imaging, because it is highly lipophilic. N-methyl-[11C]-2-(4＊-methylaminophenyl)-6-hydroxybenzothiasole, a 汕-amyloid binding compound based on a series of neutral thioflavin-T derivatives (15), was radiolabeled with the positron-emitting radionuclide 11C ([11C]6-OH-BTA-1 or [11C]PIB). [11C]6-OH-BTA-1 was found to be a promising imaging agent for the senile plaques in the brain (16). Zhang et al. (17) reported the development of a series of fluorinated polyethylene glycol (PEG) units (n = 2-5) for PET imaging of 汕-amyloid plaques in the brain. Two of them, [18F]{4-[2-(4-{2-(2[2-(2-Fluoro-ethoxy)-ethoxyl]-ethoxy}-phenyl)-vinyl]-phenyl}-methyl-amine ([18F]BAY94-9172, [18F]AV-1) (18) and (E)-4-(2-(6-(2-(2-(2-([18F]-fluoroethoxy)ethoxy)ethoxy)pyridin-3-yl)vinyl)-N-methyl benzenamine ([18F]AV-45) (19), are being evaluated in clinical trials.
5-(5-(2-(2-(2-[18F]Fluoroethoxy)ethoxy)ethoxy)benzofuran-2-yl)- N-methylbenzenamine
Alzheimer's disease (AD) is a form of dementia with a gradual memory loss and a progressive decline in mental functions over time (1, 2). It is characterized pathologically by neuronal loss, extracellular senile plaques (aggregates of amyloid-汕 peptides consisting of 40每42 amino acids), and intracellular neurofibrillary tangles (filaments of microtubule-binding hyperphosphorylated protein tau) in the brain, especially in the hippocampus and associative regions of the cortex (3, 4). 汕-Amyloid peptides and tau proteins are implicated as the main causes of neuronal degeneration and cell death (5, 6).
Early diagnosis of AD is important for treatment consideration and disease management (7). Various 汕-amyloid imaging agents have been developed for magnetic resonance imaging (MRI), single-photon emission computed tomography, and positron emission tomography (PET) (8-13) as measures of the presence of plaque. The binding of different derivatives of Congo red, thioflavin, stibene, and aminonaphthalene has been studied in human post-mortem brain tissue and in transgenic mice. Of these analogs, 2-(1-(6-[(2-[18F]fluoroethyl)(methyl)amino]-2-naphthyl)ethylidene)malono nitrile ([18F]FDDNP) was studied in humans, and it showed more binding in the brains of patients with AD than in those of healthy people (14). However, [18F]FDDNP showed low signal/noise ratios for PET imaging because it is highly lipophilic. N-Methyl-[11C]-2-(4＊-methylaminophenyl)-6-hydroxybenzothiasole, a 汕-amyloid binding compound based on a series of neutral thioflavin-T derivatives (15), was radiolabeled with the positron-emitting radionuclide 11C ([11C]6-OH-BTA-1 or [11C]PIB). [11C]6-OH-BTA-1 was found to be a promising imaging agent for senile plaques in the brain (10). 5-(5-(2-(2-(2-[18F]Fluoroethoxy)ethoxy)ethoxy)benzofuran-2-yl)-N,N-dimethylbenzenamine ([18F]FPHBF-1) was found to exhibit good initial uptake but slow washout from the brain in normal mice, and thus it is not suitable for imaging studies. Ono et al. (16) reported the development of the less lipophilic monomethylamino derivative of [18F]FPHBF-1, 5-(5-(2-(2-(2-[18F]fluoroethoxy)ethoxy)ethoxy)benzofuran-2-yl)-N-methylbenzenamine ([18F]FPHBF-2) as a PET imaging agent for 汕-amyloid plaques in the brain.
Florbetapir F 18
Information in this record refers to the use of florbetapir 18 as a diagnostic agent. No information is available on the use of florbetapir 18 during breastfeeding. The manufacturer recommends withholding breastfeeding for 24 hours after a diagnostic dose of 370 MBq (10 mCi). This length of time is greater than 10 half-lives of the radioisotope, so the nursing infant should not be exposed to radiation if this guideline is followed. The mother can nurse just before administration of the radiopharmaceutical. If the mother has expressed and saved milk prior to the examination, she can feed it to the infant during the period of nursing interruption.[1,2]
Mothers concerned about the level of radioactivity in their milk could ask to have it tested at a nuclear medicine facility at their hospital. When the radioactivity is at a safe level she may resume breastfeeding. A method for measuring milk radioactivity and determining the time when a mother can safely resume breastfeeding has been published.[3]
Whole-body biodistribution and brain PET imaging with [18F]AV-45, a novel amyloid imaging agent--a pilot study
Purpose: The compound (E)-4-(2-(6-(2-(2-(2-(18)F-fluoroethoxy)ethoxy)ethoxy) pyridin-3-yl)vinyl)-N-methylbenzenamine ([(18)F]AV-45) is a novel radiopharmaceutical capable of selectively binding to beta-amyloid (A beta) plaques. This pilot study reports the safety, biodistribution, and radiation dosimetry of [(18)F]AV-45 in human subjects.
Methods: In vitro autoradiography and fluorescent staining of postmortem brain tissue from patients with Alzheimer's disease (AD) and cognitively healthy subjects were performed to assess the specificity of the tracer. Biodistribution was assessed in three healthy elderly subjects (mean age: 60.0+/-5.2 years) who underwent 3-h whole-body positron emission tomography (PET)/computed tomographic (CT) scans after a bolus injection of 381.9+/-13.9 MBq of [(18)F]AV-45. Another six subjects (three AD patients and three healthy controls, mean age: 67.7+/-13.6 years) underwent brain PET studies. Source organs were delineated on PET/CT. All subjects underwent magnetic resonance imaging (MRI) for obtaining structural information.
Results: In vitro autoradiography revealed exquisitely high specific binding of [(18)F]AV-45 to postmortem AD brain sections, but not to the control sections. There were no serious adverse events throughout the study period. The peak uptake of the tracer in the brain was 5.12+/-0.41% of the injected dose. The highest absorbed organ dose was to the gallbladder wall (184.7+/-78.6 microGy/MBq, 4.8 h voiding interval). The effective dose equivalent and effective dose values for [(18)F]AV-45 were 33.8+/-3.4 microSv/MBq and 19.3+/-1.3 microSv/MBq, respectively.
Conclusion: [(18)F]AV-45 binds specifically to A beta in vitro, and is a safe PET tracer for studying A beta distribution in human brain. The dosimetry is suitable for clinical and research application.