Cat. No.: HY-107352

Fosfenopril

(Synonyms: Fosinoprilat; Fosinoprilic acid; SQ 27519)

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

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Pureté: 99.85%
CAS No.: 95399-71-6
Formule: C₂₃H₃₄NO₅P
Masse moléculaire:435.49

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Fosfenopril Chemical Structure

CAS No.: 95399-71-6

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

TLR4

NF-κB

IL-6

IL-1β

Voir tous les produits spécifiques à Isoform Toll-like Receptor (TLR) :

Voir tous les produits spécifiques à Isoform NF-κB :

Voir tous les produits spécifiques à Isoform TNF Receptor :

Voir tous les produits spécifiques à Isoform Interleukin Related :

In Vitro

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

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^[1]

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.

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^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Famale mongrel dogs (n=7)^[3]
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).

Chemical Information

CAS No. 95399-71-6
Appearance Solid
Masse moléculaire 435.49
Formule C₂₃H₃₄NO₅P
Color White to off-white
SMILES

O=P(CCCCC1=CC=CC=C1)(O)CC(N2C[C@H](C3CCCCC3)C[C@H]2C(O)=O)=O
Synonyms

Fosinoprilat; Fosinoprilic acid; SQ 27519
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (229.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. 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]

[2]. 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]

[3]. 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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2963 mL	11.4813 mL	22.9626 mL	57.4066 mL
	5 mM	0.4593 mL	2.2963 mL	4.5925 mL	11.4813 mL
	10 mM	0.2296 mL	1.1481 mL	2.2963 mL	5.7407 mL
	15 mM	0.1531 mL	0.7654 mL	1.5308 mL	3.8271 mL
	20 mM	0.1148 mL	0.5741 mL	1.1481 mL	2.8703 mL
	25 mM	0.0919 mL	0.4593 mL	0.9185 mL	2.2963 mL
	30 mM	0.0765 mL	0.3827 mL	0.7654 mL	1.9136 mL
	40 mM	0.0574 mL	0.2870 mL	0.5741 mL	1.4352 mL
	50 mM	0.0459 mL	0.2296 mL	0.4593 mL	1.1481 mL
	60 mM	0.0383 mL	0.1914 mL	0.3827 mL	0.9568 mL
	80 mM	0.0287 mL	0.1435 mL	0.2870 mL	0.7176 mL
	100 mM	0.0230 mL	0.1148 mL	0.2296 mL	0.5741 mL

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Fosfenopril

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Voir tous les produits spécifiques à Isoform Toll-like Receptor (TLR)

Voir tous les produits spécifiques à Isoform NF-κB

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Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Fosfenopril Related Classifications

HY-107352 Related Classifications