Fosfenopril
Based on 1 Customer Validation
Fosfenopril (Fosinoprilat) is a potent angiotensin converting enzyme (ACE) inhibitor. Fosfenopril alleviates lipopolysaccharide (LPS)-induced inflammation by inhibiting TLR4/NF-κB signaling in monocytes.
For research use only. We do not sell to patients.
- Purity: 99.85%
- CAS No.: 95399-71-6
- Formula: C23H34NO5P
- Molecular Weight:435.49
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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TLR4 |
NF-κB |
IL-6 |
IL-1β |
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.
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Cell Line:THP1 cells
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Concentration:0, 0.25, 0.5, 1, 5, and 10 μM
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Incubation Time:1 h
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Result:Down-regulated the expression of NF-κB protein.
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Cell Line:THP1 cells
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Concentration:0, 0.25, 0.5, 1, 5, and 10 μM
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Incubation Time:5 min
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Result:Showed a dose-dependent inhibitory effect on the TLR4 expression.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Famale mongrel dogs (n=7)[3]
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Dosage:0.5 mg/kg (1.1 mumol/kg) bolus plus 0.1 mg/kg/min (0.22 mumol/kg/min)
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Administration:IV, once
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Result:Increased p-aminohippurate (PAH) clearance and glomerular filtration rate (GFR) by 25 and 16%, respectively without changing arterial pressure (AP).
Chemical Information
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CAS No. 95399-71-6
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Appearance Solid
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Molecular Weight 435.49
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Formula C23H34NO5P
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Color White to off-white
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SMILES
O=P(CCCCC1=CC=CC=C1)(O)CC(N2C[C@H](C3CCCCC3)C[C@H]2C(O)=O)=O
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Synonyms
Fosinoprilat; Fosinoprilic acid; SQ 27519
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |