Fosfenopril Fosinoprilat; Fosinoprilic acid; SQ 27519|cas:95399-71-6|西域试剂

Fosfenopril Fosinoprilat; Fosinoprilic acid; SQ 27519,99.89%

产品编号：Bellancom-107352| CAS NO：95399-71-6| 分子式：C₂₃H₃₄NO₅P| 分子量：435.49

福非普利是一种有效的血管紧张素转换酶（ACE）抑制剂。福芬普利通过抑制单核细胞中TLR4/NF-κB信号传导来减轻脂多糖（LPS）诱导的炎症。

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货号	价格	库存与货期
Bellancom-107352	￥1280.00	杭州北京（现货）
Bellancom-107352	￥3800.00	杭州北京（现货）
Bellancom-107352	￥6200.00	杭州北京（现货）

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Fosfenopril Fosinoprilat; Fosinoprilic acid; SQ 27519

产品介绍

Fosfenopril (Fosinoprilat) 是一种有效的血管紧张素转换酶 (ACE) 抑制剂。Fosfenopril 通过抑制单核细胞中 TLR4/NF-κB 信号通路缓解脂多糖 (LPS) 诱导的炎症反应。

生物活性

Fosfenopril (Fosinoprilat) is a potent angiotensin converting enzyme (ACE) inhibitor. Fosfenopril alleviates lipopolysaccharide (LPS)-induced inflammation by inhibiting TLR4/NF-κB signaling in monocytes.

体外研究

Fosfenopril (0-10 μM, 5 min) inhibits the expression of TLR4 which is elevated by LPS.
Fosfenopril (0-10 μM, 1 h)attenuates the expression of NF-κB which is activated by LPS.
Fosfenopril inhibits LPS-induced cytokines (IL-6, IL-1β, and TNF-α) expression.

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

Western Blot Analysis

Cell Line:	THP1 cells
Concentration:	0, 0.25, 0.5, 1, 5, and 10 μM
Incubation Time:	1 h
Result:	Down-regulated the expression of NF-κB protein.

RT-PCR

Cell Line:	THP1 cells
Concentration:	0, 0.25, 0.5, 1, 5, and 10 μM
Incubation Time:	5 min
Result:	Showed a dose-dependent inhibitory effect on the TLR4 expression.

体内研究
(In Vivo)

Fosfenopril (0.5 mg/kg bolus plus 0.1 mg/kg/min, IV, once) increases p-aminohippurate (PAH) clearance and glomerular filtration rate (GFR) in dogs.

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

Animal Model:	Famale mongrel dogs (n=7)
Dosage:	0.5 mg/kg (1.1 mumol/kg) bolus plus 0.1 mg/kg/min (0.22 mumol/kg/min)
Administration:	IV, once
Result:	Increased p-aminohippurate (PAH) clearance and glomerular filtration rate (GFR) by 25 and 16%, respectively without changing arterial pressure (AP).

体内研究

Fosfenopril (0.5 mg/kg bolus plus 0.1 mg/kg/min, IV, once) increases p-aminohippurate (PAH) clearance and glomerular filtration rate (GFR) in dogs.

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

Animal Model:	Famale mongrel dogs (n=7)
Dosage:	0.5 mg/kg (1.1 mumol/kg) bolus plus 0.1 mg/kg/min (0.22 mumol/kg/min)
Administration:	IV, once
Result:	Increased p-aminohippurate (PAH) clearance and glomerular filtration rate (GFR) by 25 and 16%, respectively without changing arterial pressure (AP).

体内研究

Fosfenopril (0.5 mg/kg bolus plus 0.1 mg/kg/min, IV, once) increases p-aminohippurate (PAH) clearance and glomerular filtration rate (GFR) in dogs.

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

Animal Model:	Famale mongrel dogs (n=7)
Dosage:	0.5 mg/kg (1.1 mumol/kg) bolus plus 0.1 mg/kg/min (0.22 mumol/kg/min)
Administration:	IV, once
Result:	Increased p-aminohippurate (PAH) clearance and glomerular filtration rate (GFR) by 25 and 16%, respectively without changing arterial pressure (AP).

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (229.63 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2963 mL	11.4813 mL	22.9626 mL
5 mM	0.4593 mL	2.2963 mL	4.5925 mL
10 mM	0.2296 mL	1.1481 mL	2.2963 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: ≥ 2.5 mg/mL (5.74 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.74 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.74 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.74 mM，饱和度未知) 的澄清溶液。
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 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: ≥ 2.5 mg/mL (5.74 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.74 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。

*以上所有助溶剂都可在西域网站选购。

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

参考文献

. Yang S, et al. Fosinoprilat alleviates lipopolysaccharide (LPS)-induced inflammation by inhibiting TLR4/NF-κB signaling in monocytes. Cell Immunol. 2013 Jul-Aug;284(1-2):182-6. [Content Brief]

. DeForrest JM, et al. Fosinopril, a phosphinic acid inhibitor of angiotensin I converting enzyme: in vitro and preclinical in vivo pharmacology. J Cardiovasc Pharmacol. 1989 Nov;14(5):730-6. [Content Brief]

. DeForrest JM, et al. Blood pressure lowering and renal hemodynamic effects of fosinopril in conscious animal models. J Cardiovasc Pharmacol. 1990 Jul;16(1):139-46. [Content Brief]

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产品编号(Item Number)

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Fosfenopril Fosinoprilat; Fosinoprilic acid; SQ 27519,99.89%

Fosfenopril Fosinoprilat; Fosinoprilic acid; SQ 27519

化学品安全说明书(MSDS)

质检证书(COA)

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