| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
TLR4 expression induced by LPS is inhibited by fosfenopril (0–10 μM, 5 minutes) [1]. LPS-activated NF-κB expression can be attenuated by fosfenopril (0–10 μM, 1 h) [1]. LPS-induced cytokine (IL-6, IL-1β, and TNF-α) expression is inhibited by fosfenopril [1].
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|---|---|
| ln Vivo |
Dogs' glomerular filtration rate (GFR) and clearance of paraaminohippuric acid (PAH) are both increased by forfenopril (0.5 mg/kg bolus plus 0.1 mg/kg/min IV once) [3].
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| Cell Assay |
Western Blot analysis [1]
Cell Types: THP1 Cell Tested Concentrations: 0, 0.25, 0.5, 1, 5, 10 μM Incubation Duration: 1 h Experimental Results: NF-κB protein expression was down-regulated. RT-PCR[1] Cell Types: THP1 Cell Tested Concentrations: 0, 0.25, 0.5, 1, 5 and 10 μM Incubation Duration: 5 minutes Experimental Results: Dose-dependent inhibition of TLR4 expression. |
| Animal Protocol |
Animal/Disease Models: Female Mongrel Dog (n=7)[3]
Doses: 0.5 mg/kg (1.1 mumol/kg) bolus plus 0.1 mg/kg/min (0.22 mumol/kg/min) Route of Administration: IV, one result Experimental Results: Increases para-aminohippuric acid (PAH) clearance and glomerular filtration rate (GFR) by 25% and 16% respectively without changing arterial pressure (AP). |
| References |
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| Additional Infomation |
Fosinoprilat is a phosphinic acid-containing N-acyl derivative of (4S)-cyclohexyl-L-proline. An inhibitor of angiotensin converting enzyme (ACE), it is used as the phosphinate ester pro-drug fosinopril for treatment of hypertension and chronic heart failure. It has a role as an antihypertensive agent and an EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor. It is a member of phosphinic acids and a L-proline derivative.
Fosinoprilat is the active phosphinic acid metabolite of prodrug [fosinopril], which is activated by esterases in vivo. It binds zinc with phosphinic acid group. Fosinoprilat is an Angiotensin Converting Enzyme Inhibitor. The mechanism of action of fosinoprilat is as an Angiotensin-converting Enzyme Inhibitor. Fosinoprilat is a phosphinic acid-containing angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Fosinoprilat specifically and competitively inhibits angiotensin-converting enzyme thereby decreasing the formation of the potent vasoconstrictor angiotensin II, resulting in diminished vasopressor activity. In addition, angiotensin II-mediated aldosterone secretion by adrenal cortex is decreased, which results in a decrease of sodium retention and an increase in water outflow. See also: Fosinopril (is active moiety of); Fosinopril Sodium (active moiety of). |
| Molecular Formula |
C23H34NO5P
|
|---|---|
| Molecular Weight |
435.5
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| Exact Mass |
435.217
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| CAS # |
95399-71-6
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| Related CAS # |
Fosfenopril-d7;1279220-43-7
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| PubChem CID |
62956
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| Appearance |
White to off-white solid powder
|
| Density |
1.238g/cm3
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| Boiling Point |
728.9ºC at 760mmHg
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| Melting Point |
>300ºC
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| Flash Point |
394.6ºC
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| Index of Refraction |
1.564
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| LogP |
4.099
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
30
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| Complexity |
627
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| Defined Atom Stereocenter Count |
2
|
| SMILES |
C1CCC(CC1)[C@@H]2C[C@H](N(C2)C(=O)CP(=O)(CCCCC3=CC=CC=C3)O)C(=O)O
|
| InChi Key |
WOIWWYDXDVSWAZ-RTWAWAEBSA-N
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| InChi Code |
InChI=1S/C23H34NO5P/c25-22(17-30(28,29)14-8-7-11-18-9-3-1-4-10-18)24-16-20(15-21(24)23(26)27)19-12-5-2-6-13-19/h1,3-4,9-10,19-21H,2,5-8,11-17H2,(H,26,27)(H,28,29)/t20-,21+/m1/s1
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| Chemical Name |
(2S,4S)-4-cyclohexyl-1-[2-[hydroxy(4-phenylbutyl)phosphoryl]acetyl]pyrrolidine-2-carboxylic acid
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| Synonyms |
SQ-27,519; SQ 27,519; Fosinoprilat
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~229.63 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.74 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.74 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2962 mL | 11.4811 mL | 22.9621 mL | |
| 5 mM | 0.4592 mL | 2.2962 mL | 4.5924 mL | |
| 10 mM | 0.2296 mL | 1.1481 mL | 2.2962 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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