BrBzGCp2 (Synonyms: S-p-Bromobenzylglutathione cyclopentyl diester) |
| رقم الكتالوجGC61398 |
BrBzGCp2 هو مثبط Glyoxalase 1 (GLO1) ، مع GC50 من 4.23 ميكرومتر في خلايا HL-60
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 166038-00-2
Sample solution is provided at 25 µL, 10mM.
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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 | |
| المرادفات | 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 | ||
| Formula | C27H38BrN3O6S | M.Wt | 612.58 |
| الذوبان | DMSO: 250 mg/mL (408.11 mM) | Storage | -20°C, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6324 mL | 8.1622 mL | 16.3244 mL |
| 5 mM | 326.5 μL | 1.6324 mL | 3.2649 mL |
| 10 mM | 163.2 μL | 816.2 μL | 1.6324 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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