BrBzGCp2(Synonyms: S-p-Bromobenzylglutathione cyclopentyl diester)

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BrBzGCp2 (Synonyms: S-p-Bromobenzylglutathione cyclopentyl diester) 纯度: 98.88%

BrBzGCp2 是乙二醛酶 1 (GLO1) 的抑制剂，其 GC50 为 4.23 μM (HL-60 细胞)。BrBzGCp2 具有抗肿瘤和神经保护活性。

BrBzGCp2(Synonyms: S-p-Bromobenzylglutathione cyclopentyl diester)

BrBzGCp2 Chemical Structure

CAS No. : 166038-00-2

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10 mM * 1 mL in DMSO ￥1080 In-stock
5 mg ￥800 In-stock
10 mg ￥1400 In-stock
25 mg ￥3000 In-stock
50 mg ￥5000 In-stock
100 mg ￥8000 In-stock
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BrBzGCp2 相关产品

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生物活性

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].
体内研究
(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 GABAA receptor activation[4].
BrBzGCp2 significantly lowers the blood pressure and ameliorated endothelial dysfunction in diabetic mice[5].

上海金畔生物科技有限公司 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

分子量

612.58

Formula

C27H38BrN3O6S
CAS 号

166038-00-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, stored under nitrogen

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

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

配制储备液
浓度 溶剂体积 质量 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： 8% DMSO    18% Tween-80    74% saline

    Solubility: 20 mg/mL (32.65 mM); Suspended solution; Need ultrasonic

  • 2.

    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

    此方案可获得 ≥ 2.08 mg/mL (3.40 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

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

    此方案可获得 ≥ 2.08 mg/mL (3.40 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [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.

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