Fiboflapon - CAS:936350-00-4

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Fiboflapon (Synonyms:GSK2190915; AM-803)

目录号 : KM9332 CAS No. : 936350-00-4 纯度 : 98%

产品说明书产品使用指南

Fiboflapon (GSK2190915; AM-803) 是一种口服有效的 5-脂氧合酶激活蛋白 (FLAP) 抑制剂，结合 FLAP 的效价为 2.9 nM，在人血中抑制 LTB4 的 IC₅₀ 为 76 nM。

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5mg		In-stock
10mg		In-stock
50mg		In-stock
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200mg	询价	In-stock

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生物活性

Fiboflapon (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC₅₀ of 76 nM for inhibition of LTB4 in human blood.

体外研究

Fiboflapon (AM-803) exhibits excellent preclinical toxicology and pharmacokinetics in rat and dog. Fiboflapon (AM-803) also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model [1].

体内研究

Oral administration of Fiboflapon (AM-803: 1 mg/kg) results in sustained inhibition of ex vivo ionophore-challenged whole blood LTB4 biosynthesis with >90% inhibition for up to 12 h and an EC₅₀ of approximately 7 nM. When rat lungs are challenged in vivo with calcium-ionophore, Fiboflapon (AM-803) inhibits LTB4 and cysteinyl leukotriene (CysLT) production with ED₅₀s of 0.12 mg/kg and 0.37 mg/kg, respectively. The inhibition measured 16 h following a single oral dose of 3 mg/kg was 86% and 41% for LTB4 and CysLTs, respectively. In an acute inflammation setting, Fiboflapon dose-dependently reduced LTB4, CysLTs, plasma protein extravasation and neutrophil influx induced by peritoneal zymosan injection. Finally, Fiboflapon increases survival time in mice exposed to a lethal intravenous injection of platelet activating factor (PAF).

分子式

C₃₈H₄₃N₃O₄S

分子量

637.83

CAS号

936350-00-4

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 : 50 mg/mL (78.39 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5678 mL	7.8391 mL	15.6782 mL
5 mM	0.3136 mL	1.5678 mL	3.1356 mL
10 mM	0.1568 mL	0.7839 mL	1.5678 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% corn oil
Solubility: ≥ 2.5 mg/mL (3.92 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.92 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。