FK706|cas:144055-55-0|西域试剂

FK706,99.57%

产品编号：Bellancom-19269| CAS NO：144055-55-0| 分子式：C₂₆H₃₂F₃N₄NaO₇| 分子量：592.54

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-19269	￥4700.00	杭州北京（现货）
Bellancom-19269	￥7500.00	杭州北京（现货）
Bellancom-19269	￥15000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

FK706

产品介绍

FK706 是一种有效，缓慢结合和竞争性的人中性粒细胞弹性蛋白酶抑制剂，IC₅₀ 为 83 nM，K_i 为 4.2 nM。FK706 还抑制小鼠中性粒细胞弹性蛋白酶和猪胰弹性蛋白酶，IC₅₀ 分别为 22 nM 和 100 nM，并且对其他丝氨酸蛋白酶 (例如人胰胰蛋白酶，人胰腺α-胰凝乳蛋白酶和人白细胞组织蛋白酶G) 没有抑制活性。FK706 具有抗炎作用。

生物活性

FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC₅₀ of 83 nM and a K_i of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC₅₀s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect.

体外研究

FK706 effectively inhibits the hydrolysis of bovine neck ligament elastin (2 mg/mL final concentration) by human neutrophil elastase (4 μg/mL final concentration) with an IC50 value of 230 nM.
FK706 blocks the release of inflammatory chemokines, suppresses the expression of IL-8 and MCP-1 mRNA, and suppresses NF-κB activation. It seems possible that FK706 may directly blocks human lung fibroblasts activation of NF-κB, preventing expression of inflammatory chemokines during cigarette smoke–induced lung inflammation.

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

体内研究

FK706 (10-100 mg/kg; subcutaneous injection; for 1-6 hours; male C57BL mice) treatment significantly suppresses human neutrophil elastase (20 μg/paw)-induced paw edema in mice in a dose-dependent manner (47% inhibition at a dose of 100 mg/kg).

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

Animal Model:	Male C57BL mice (6 weeks old) injected with human neutrophil elastase
Dosage:	10 mg/kg, 32 mg/kg, 100 mg/kg
Administration:	Subcutaneous injection; for 1 hour, 2 hours, 4 hours, 6 hours
Result:	Significantly suppressed human neutrophil elastase-induced paw edema in mice in a dose-dependent manner.

体内研究

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

Animal Model:	Male C57BL mice (6 weeks old) injected with human neutrophil elastase
Dosage:	10 mg/kg, 32 mg/kg, 100 mg/kg
Administration:	Subcutaneous injection; for 1 hour, 2 hours, 4 hours, 6 hours
Result:	Significantly suppressed human neutrophil elastase-induced paw edema in mice in a dose-dependent manner.

性状

Solid

溶解性数据

In Vitro:

DMSO : 115 mg/mL (194.08 mM; Need ultrasonic)

H₂O : ≥ 100 mg/mL (168.76 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	1.6876 mL	8.4382 mL	16.8765 mL
5 mM	0.3375 mL	1.6876 mL	3.3753 mL
10 mM	0.1688 mL	0.8438 mL	1.6876 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 (sealed storage, away from moisture)。-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: ≥ 5 mg/mL (8.44 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (8.44 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (8.44 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (8.44 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (8.44 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (8.44 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 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。