OGT 2115

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OGT 2115  纯度: 98.09%

OGT 2115 是一种有效的，细胞可渗透且口服活性的乙酰肝素酶 (heparanase) 抑制剂，IC50 为 0.4 μM。OGT 2115 具有抗血管生成特性 (IC50 为 1 μM)。OGT 2115 还抑制硫酸乙酰肝素的降解活性。

OGT 2115

OGT 2115 Chemical Structure

CAS No. : 853929-59-6

规格 价格 是否有货 数量
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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OGT 2115 相关产品

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生物活性

OGT 2115 is a potent, cell-permeable and orally active heparanase inhibitor with an IC50 of 0.4 μM. OGT 2115 has anti-angiogenic properties (IC50 of 1 μM). OGT 2115 also inhibits heparan sulfate degradation activity[1][2].

IC50 & Target

IC50: 0.4 μM (Heparanase)[1]
体外研究
(In Vitro)

Heparanase InhibitorOGT 2115 can suppress metastasis induced by endoplasmic reticulum (ER) stress in breast cancer cells, although not significantly. However, compared with the control group, the number and rate of migrated cells are significantly reduced following the exposure of the cells to Tunicamycin + OGT 2115. OGT 2115 significantly inhibits the invasion and migration induced by Adriamycin. Furthermore, the MTT assay results show that OGT 2115 does not decrease the anti-proliferative effect of Adriamycin[2].

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.
体内研究
(In Vivo)

When administered to mice, OGT 2115 (Compound 12d) shows a plasma concentration of ~10x the heparanase IC50 following oral dosing at 20 mg/kg[1].

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.
分子量

495.30

Formula

C24H16BrFN2O4
CAS 号

853929-59-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 11.36 mg/mL (22.94 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0190 mL 10.0949 mL 20.1898 mL
5 mM 0.4038 mL 2.0190 mL 4.0380 mL
10 mM 0.2019 mL 1.0095 mL 2.0190 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。-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： 0.5% CMC-Na/saline water

    Solubility: 10 mg/mL (20.19 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 1.14 mg/mL (2.30 mM); Clear solution

    此方案可获得 ≥ 1.14 mg/mL (2.30 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 11.4 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]. [1]Courtney SM, et al. Furanyl-1,3-thiazol-2-yl and benzoxazol-5-yl acetic acid derivatives: novel classes of heparanase inhibitor. Bioorg Med Chem Lett. 2005 May 2;15(9):2295-9.

    [2]. Li Y, et al. Suppression of endoplasmic reticulum stress-induced invasion and migration of breast cancer cells through the downregulation of heparanase. Int J Mol Med. 2013 May;31(5):1234-42.

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