BAY-876 | whatman (沃特曼)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

BAY-876 纯度: 98.05%

BAY-876 是一种具有口服活性的，选择性的葡萄糖转运蛋白 1 (GLUT1) 抑制剂，IC₅₀ 为 2 nM。BAY-876 对 GLUT1 的选择性是 GLUT2，GLUT3 和 GLUT4 的 130 倍以上。BAY-876 还是一种糖酵解代谢和卵巢癌生长的有效阻滞剂。

BAY-876 Chemical Structure

CAS No. : 1799753-84-6

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1529	In-stock
2 mg	￥990	In-stock
5 mg	￥1400	In-stock
10 mg	￥2200	In-stock
50 mg	￥7100	In-stock
100 mg	￥11000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

BAY-876 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Membrane Transporter/Ion Channel Compound Library
Anti-Cancer Compound Library
Glycolysis Compound Library
Orally Active Compound Library
Chemical Probe Library
Glutamine Metabolism Compound Library
Anti-Cancer Metabolism Compound Library
Glucose Metabolism Compound Library
Targeted Diversity Library

生物活性

BAY-876 is an orally active and selective glucose transporter 1 (GLUT1) inhibitor with an IC₅₀ of 2 nM. BAY-876 is >130-fold more selective for GLUT1 than GLUT2, GLUT3, and GLUT4^[1]. BAY-876 is also a potent blocker of glycolytic metabolism and ovarian cancer growth^[2].

IC₅₀ & Target^[1]

GLUT1

2 nM (IC₅₀)

GLUT2

10.08 μM (IC₅₀)

GLUT3

1.67 μM (IC₅₀)

GLUT4

0.29 μM (IC₅₀)

体外研究
(In Vitro)

BAY-876 (25-75 nM; 24 and 72 hours) has the growth-inhibitory effect and leads to a dose-dependent decrease in numbers of SKOV-3 and OVCAR-3 cells^[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.

Cell Proliferation Assay^[2]

Cell Line:	SKOV-3 and OVCAR-3 cells
Concentration:	25, 50, 75 nM
Incubation Time:	24 and 72 hours
Result:	Led to a dose-dependent decrease in numbers of SKOV-3 and OVCAR-3 cells.

体内研究
(In Vivo)

BAY-876 (oral administration; 1.5-4.5 mg/kg/day for 28 days) causes a clear dose-dependent inhibition of tumorigenicity in mice^[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.

Animal Model:	Female NOD-scid IL2rg^null (NSG) mice carrying SKOV-3 subcutaneous (s.c.) xenografts^[2]
Dosage:	1.5, 3, 4.5 mg/kg
Administration:	Oral administration; daily; for 28 days
Result:	Caused a clear dose-dependent inhibition of tumorigenicity.

分子量

496.42

Formula

C₂₄H₁₆F₄N₆O₂

CAS 号

1799753-84-6

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 : ≥ 100 mg/mL (201.44 mM)

Methanol : 1 mg/mL (2.01 mM; ultrasonic and warming and heat to 60°C)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0144 mL	10.0721 mL	20.1442 mL
5 mM	0.4029 mL	2.0144 mL	4.0288 mL
10 mM	0.2014 mL	1.0072 mL	2.0144 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： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (5.04 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.04 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 25.0 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.04 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.04 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 25.0 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]. Siebeneicher H et al. Identification and Optimization of the First Highly Selective GLUT1 Inhibitor BAY-876. ChemMedChem. 2016 Aug 23.

[2]. Ma Y, et al. Ovarian Cancer Relies on Glucose Transporter 1 to Fuel Glycolysis and Growth: Anti-Tumor Activity of BAY-876. Cancers (Basel). 2018 Dec 31;11(1).

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