BrBzGCp2-武汉科斯坦生物科技有限公司

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BrBzGCp2

英文名称：BrBzGCp2

品牌：Chemstan

货号：CS-136684

cas：166038-00-2

价格： ￥800/mg
发布日期： 2021-03-10
更新日期： 2025-09-19

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产地
品牌	Chemstan
货号	CS-136684
用途	科研
英文名称	BrBzGCp2
包装规格	5 mg
纯度	98%%
CAS编号	166038-00-2
别名
分子式
是否进口	否

Description

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].

IC₅₀ & Target

GC50: 4.23 μM (GLO1)^[1].

In Vivo

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 GABA_A receptor activation^[4].
BrBzGCp2 significantly lowers the blood pressure and ameliorated endothelial dysfunction in diabetic mice^[5].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male CD-1 mice^[2].
Dosage:	50 mg/kg.
Administration:	IP once (Two hours post-injection, mice were sacrificed, and brains were rapidly dissected and flash-frozen on dry ice. MG concentration was measured)
Result:	Allowed MG levels to accumulate for 2 hours

Molecular Weight

612.58

Formula

C??H??BrN?O?S

CAS No.

166038-00-2

SMILES

O=C(NCC(OC1CCCC1)=O)[C@@H](NC(CC[C@H](N)C(OC2CCCC2)=O)=O)CSCC(C=C3)=CC=C3Br

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (408.11 mM; Need ultrasonic)

Preparing
Stock Solutions

ConcentrationSolventMass	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

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, 6 months; -20°C, 1 month (stored under nitrogen)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (3.40 mM); Clear solution
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.40 mM); Clear solution

*以上所有助溶剂都可在 MCE 网站选购。

References

[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.