GW274150 phosphate|cas:438542-15-5|西域试剂

GW274150 phosphate,99.85%

产品编号：Bellancom-12119A| CAS NO：438542-15-5| 分子式：C₈H₂₀N₃O₆PS| 分子量：317.30

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-12119A	￥900.00	杭州北京（现货）
Bellancom-12119A	￥1500.00	杭州北京（现货）
Bellancom-12119A	￥3100.00	杭州北京（现货）
Bellancom-12119A	￥5000.00	杭州北京（现货）
Bellancom-12119A	￥8000.00	杭州北京（现货）

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GW274150 phosphate

产品介绍

GW274150 phosphate 是一种有效的，选择性的，口服活性的 NADPH 依赖型人诱导型一氧化氮合成酶 (iNOS) (K_d=40 nM) 和大鼠 (iNOS) 抑制剂。GW274150 phosphate 对人和大鼠内皮一氧化氮合酶 (eNOS) 和神经元一氧化氮合酶 (nNOS) 均显示较低效力。GW274150 phosphate 在急性肺损伤炎症模型中发挥保护作用。

生物活性

GW274150 phosphate is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC₅₀=2.19 μM; K_d=40 nM) and rat iNOS (ED₅₀=1.15 μM). GW274150 phosphate displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 phosphate exerts a protective role in an acute model of lung injury inflammation.

体外研究

GW274150 phosphate inhibits intracellular iNOS in J774 cells in a time-dependent manner, reaching IC₅₀ values of 0.2±0.04 μM.
GW274150 is >260-fold and 219-fold selective for iNOS against eNOS and nNOS in rat tissues, respectively. And it displays >100-fold and >80-fold for human iNOS against human eNOS and nNOS, respectively.

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

体内研究

GW274150 phosphate is a long-acting (5 h half‐life in rats) iNOS inhibitor and is able to inhibit LPS‐mediated increase in plasma NO2^-, NO3^- levels 14 h after single intraperitoneal dose (ED₅₀=3 mg/kg).
GW274150 phosphate (intraperitoneal injection; 2.5, 5, and 10 mg/kg; before carrageenan injection) reduces the degree of lung injury induced by carrageenan in a dose-related fashion. Oedema formation and PMNs infiltration in the pleural cavity are also significantly attenuated in a dose‐related manner in rats.
GW274150 phosphate (oral adminstration; 30 mg/kg; twice daily; 7 days) leads to significant neuroprotection, however, it displays a bell-shaped neuroprotective profile, being ineffective at high doses in 6-OHDA rat model of Parkinson disease (PD).

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

Animal Model:	SD rat
Dosage:	2.5, 5 and 10 mg/kg
Administration:	Intraperitoneal injection 5 min before carrageenan injection
Result:	Exerted a protective role in an acute model of inflammation, carrageenan-induced lung injury.

体内研究

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

Animal Model:	SD rat
Dosage:	2.5, 5 and 10 mg/kg
Administration:	Intraperitoneal injection 5 min before carrageenan injection
Result:	Exerted a protective role in an acute model of inflammation, carrageenan-induced lung injury.

性状

Solid

溶解性数据

In Vitro:

H₂O : 100 mg/mL (315.16 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1516 mL	15.7580 mL	31.5159 mL
5 mM	0.6303 mL	3.1516 mL	6.3032 mL
10 mM	0.3152 mL	1.5758 mL	3.1516 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