NE 52-QQ57|cas:1401728-56-0|西域试剂

NE 52-QQ57,99.56%

产品编号：Bellancom-101784| CAS NO：1401728-56-0| 分子式：C₂₄H₂₈N₆O| 分子量：416.52

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货号	价格	库存与货期
Bellancom-101784	￥3700.00	杭州北京（现货）
Bellancom-101784	￥6300.00	杭州北京（现货）
Bellancom-101784	￥17000.00	杭州北京（现货）

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NE 52-QQ57

产品介绍

NE 52-QQ57 是选择性，有口服活性的 GPR4 拮抗剂，IC₅₀为70 nM。NE 52-QQ57 具有抗炎活性。

生物活性

NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC₅₀ of 70 nM. NE 52-QQ57 has anti-inflammatory activity.

体外研究

NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation (IC₅₀ 26.8 nM in HEK293 cells).

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

体内研究

NE 52-QQ57 (Compound 13) shows a significant anti-inflammatory effect in the rat antigen induced arthritis model after oral administration at 30 mg/kg bid for 20 days. NE 52-QQ57 (30 mg/kg bid po for 4 days) also prevents angiogenesis in the mouse chamber model as well as pain as demonstrated in the rat complete Freund’s adjuvant model.

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

Animal Model:	Female FVB mice (8-10 weeks)
Dosage:	30 mg/kg
Administration:	Oral, 4 days, bid
Result:	Treatment at 30 mg/kg p.o. bid starting on day 0, the day of the chamber implantation, showed a statistically significant reduction (46.8±10.6%) of tissue growth by day 4. The blood levels of 13 on day 4 at 2 and 16 h after compound application in this model were 9.03±2.87 and 0.09±0.06 μM.

Animal Model:	Male Wistar Han rats
Dosage:	3, 10, and 30 mg/kg
Administration:	Oral, 20 days, bid
Result:	Displayed not only higher exposures in the rat AIA but also lower plasma protein binding in rat (95%).

体内研究

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

Animal Model:	Female FVB mice (8-10 weeks)
Dosage:	30 mg/kg
Administration:	Oral, 4 days, bid
Result:	Treatment at 30 mg/kg p.o. bid starting on day 0, the day of the chamber implantation, showed a statistically significant reduction (46.8±10.6%) of tissue growth by day 4. The blood levels of 13 on day 4 at 2 and 16 h after compound application in this model were 9.03±2.87 and 0.09±0.06 μM.

Animal Model:	Male Wistar Han rats
Dosage:	3, 10, and 30 mg/kg
Administration:	Oral, 20 days, bid
Result:	Displayed not only higher exposures in the rat AIA but also lower plasma protein binding in rat (95%).

性状

Solid

溶解性数据

In Vitro:

DMSO : 20 mg/mL (48.02 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4008 mL	12.0042 mL	24.0085 mL
5 mM	0.4802 mL	2.4008 mL	4.8017 mL
10 mM	0.2401 mL	1.2004 mL	2.4008 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 mg/mL (4.80 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (4.80 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 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% (20% SBE-β-CD in saline)
Solubility: ≥ 2 mg/mL (4.80 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (4.80 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.0 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2 mg/mL (4.80 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (4.80 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 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。