BrBzGCp2
(Synonyms: S-p-Bromobenzylglutathione cyclopentyl diester) 目录号 : GC61398
BrBzGCp2是乙二醛酶1(GLO1)的抑制剂，其GC50为4.23μM(HL-60细胞)。BrBzGCp2具有抗肿瘤和神经保护活性。
Cas No.:166038-00-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
BrBzGCp2 is a Glyoxalase 1 (GLO1) inhibitor, with a GC50 of 4.23 μM in HL-60 cells. BrBzGCp2 possesses antitumor and neuroprotective activity[1][2].
GLO1 inhibition by BrBzGCp2 increases center time in the OF test, without changing distance traveled. GLO1 inhibition increases MG (methylglyoxal) concentration, thus reducing anxiety-like behavior[2]. BrBzGCp2 pre-treatment decreases seizure duration[3].BrBzGCp2 injection alleviates the level of anxiety in mice, and mice with less anxiety and fear were more likely to explore the unknown area, implying that inhibition of GLO1 activity mitigated anxiety levels[4].BrBzGCp2 treatment restores the VPA-induced inhibition effect on GABAA receptor activation[4].BrBzGCp2 significantly lowers the blood pressure and ameliorated endothelial dysfunction in diabetic mice[5]. Animal Model: Male CD-1 mice[2].
[1]. P J Thornalley, et al. Antitumor activity of S-(p-bromobenzyl)glutathione diesters in vitro: a structure-activity study. J Med Chem. 1996 Aug 16;39(17):3409-11. [2]. Margaret G Distler, et al. Glyoxalase 1 increases anxiety by reducing GABAA receptor agonist methylglyoxal. J Clin Invest. 2012 Jun;122(6):2306-15. [3]. Katherine M. J. McMurray, et al. GLO1 inhibitors for neuropsychiatric and anti-epileptic drug development. Biochem Soc Trans. 2014 Apr;42(2):461-7. [4]. Margaret G Distler, et al. Glyoxalase 1 and its substrate methylglyoxal are novel regulators of seizure susceptibility. Epilepsia. 2013 Apr;54(4):649-57. [5]. Tao Xu, et al. GW29-e0826 ARC Regulates Programmed Necrosis and Myocardial Ischemia/Reperfusion Injury through Preventing the Opening of mPTP. J Am Coll Cardiol. 2018 Oct, 72 (16_Supplement) C27.
| Cas No. | 166038-00-2 | SDF | |
| 别名 | S-p-Bromobenzylglutathione cyclopentyl diester | ||
| Canonical SMILES | O=C(NCC(OC1CCCC1)=O)[C@@H](NC(CC[C@H](N)C(OC2CCCC2)=O)=O)CSCC(C=C3)=CC=C3Br | ||
| 分子式 | C27H38BrN3O6S | 分子量 | 612.58 |
| 溶解度 | DMSO: 250 mg/mL (408.11 mM) | 储存条件 | -20°C, stored under nitrogen |
| 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 | 1.6324 mL | 8.1622 mL | 16.3244 mL |
| 5 mM | 0.3265 mL | 1.6324 mL | 3.2649 mL |
| 10 mM | 0.1632 mL | 0.8162 mL | 1.6324 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。
Glyoxalase 1 Inhibitor Alleviates Autism-like Phenotype in a Prenatal Valproic Acid-Induced Mouse Model
ACS Chem Neurosci 2020 Nov 18;11(22):3786-3792.PMID:33166134DOI:10.1021/acschemneuro.0c00482
Autism spectrum disorder (ASD) is a severe neurological and developmental disorder that impairs a person's ability to socialize and communicate and affects behavior. The number of patients diagnosed with ASD has risen rapidly. However, the pathophysiology of ASD is poorly understood, and drugs for ASD treatment are strikingly limited. This study aims to evaluate the roles of glyoxalase 1 (GLO1)-methylglyoxal (MG)-γ-aminobutyric acid (GABA) signaling in ASD using a valproic acid (VPA)-induced animal model of autism. The GLO1 levels were analyzed by RT-qPCR and Western blot assay, and MG levels were measured with a Methylglyoxal Assay Kit. The open-field and sniff duration tests were used to assess the interest and anxiety of VPA mice. The three-chamber, marble-burying, and tail-flick tests were applied to determine the sociability, repetitive behavior, and nociceptive threshold of VPA mice. Our results demonstrated that increased GLO1 and decreased MG were observed in VPA mice. Administration of S-p-bromobenzylglutathione cyclopentyl diester (BrBzGCp2), a GLO1 inhibitor, was beneficial for alleviating anxiety, reducing repetitive behavior, and improving the impaired sociability and nociceptive threshold of VPA mice. BrBzGCp2 treatment may be developed as a promising therapeutic strategy for patients with ASD.