BAY-218 AHR antagonist 1|cas:2162982-11-6|西域试剂

BAY-218 AHR antagonist 1,99.91%

产品编号：Bellancom-111449| CAS NO：2162982-11-6| 分子式：C₂₀H₁₇ClFN₃O₃| 分子量：401.82

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货号	价格	库存与货期
Bellancom-111449	￥750.00	杭州北京（现货）
Bellancom-111449	￥1300.00	杭州北京（现货）
Bellancom-111449	￥2900.00	杭州北京（现货）
Bellancom-111449	￥4900.00	杭州北京（现货）
Bellancom-111449	￥8500.00	杭州北京（现货）

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BAY-218 AHR antagonist 1

产品介绍

BAY-218 (AHR antagonist 1) 是一种芳烃受体 (AHR) 拮抗剂。 BAY-218 在 U87 胶质母细胞瘤细胞中具有 AHR 抑制活性，IC₅₀ 为 39.9 μM。BAY-218 可用于研究癌症或免疫反应失调的病症。

生物活性

BAY-218 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist. BAY-218 has AHR inhibitory activity with an IC₅₀ of 39.9 μM in in U87 glioblastoma cells. BAY-218 can be used for the research of cancer or conditions with dysregulated immune responses.

体外研究

BAY-218 (example 23) (72 pM-20 μM) has AHR inhibitory activity with an IC₅₀ of 39.9 μM in in U87 glioblastoma cells.
BAY-218 (1 nM-3 μM) has CYP1A1 inhibitory activity with an IC₅₀ of 70.7 μM in human monocytic U937 cell line.
BAY-218 (1 μM) reverses KA-induced inhibition of TNFα production by LPS stimulated human monocytes.

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

RT-PCR

Cell Line:	human monocytic U937 cells
Concentration:	1 nM-3 μM
Incubation Time:
Result:	Regulated antagonise ligand-induced AHR gene in a dose-dependent manner.

体内研究
(In Vivo)

BAY-218 (example 23) (p.o; 30 mg/kg; bid) has good anti-tumor effect combinated with aPD-L1.

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

Animal Model:	Balb/c mice (subcutaneously CT26 cells)
Dosage:	30 mg/kg
Administration:	p.o, bid
Result:	Significantly decreased tumors size combinated with aPD-L1.

体内研究

BAY-218 (example 23) (p.o; 30 mg/kg; bid) has good anti-tumor effect combinated with aPD-L1.

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

Animal Model:	Balb/c mice (subcutaneously CT26 cells)
Dosage:	30 mg/kg
Administration:	p.o, bid
Result:	Significantly decreased tumors size combinated with aPD-L1.

体内研究

BAY-218 (example 23) (p.o; 30 mg/kg; bid) has good anti-tumor effect combinated with aPD-L1.

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

Animal Model:	Balb/c mice (subcutaneously CT26 cells)
Dosage:	30 mg/kg
Administration:	p.o, bid
Result:	Significantly decreased tumors size combinated with aPD-L1.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 250 mg/mL (622.17 mM)

* "≥" 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	2.4887 mL	12.4434 mL	24.8868 mL
5 mM	0.4977 mL	2.4887 mL	4.9774 mL
10 mM	0.2489 mL	1.2443 mL	2.4887 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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.18 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.18 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 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.18 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.18 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。