| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Eprosartan (formerly SKF-108566J; SKF108566; SKF 108566; Teveten; Futuran; Navixen; Regulaten) is a nonpeptide angiotensin II receptor antagonist that has been approved as an antihypertensive medication for the treatment of high blood pressure. It blocks angiotensin II receptor with an IC50 of 9.2 and 3.9 nM in rat and human adrenal cortical membranes, respectively.
| ln Vitro |
Eprosartan (SKF-108566J) blocks the binding of [125I]AII to the membranes of the rat mesenteric artery (IC50 of 1.5 nM) and human liver (IC50 of 1.7 nM). Eprosartan inhibited the concentration-dependent increases in intracellular Ca2+ levels induced by AII in rabbit aortic smooth muscle cells[1].
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| ln Vivo |
Eprosartan (0.01-0.3 mg/kg) administered intravenously caused dose-dependent parallel shifts in the AII pressor dose-response curve in conscious normotensive rats. When conscious normotensive rats were given Eprosartan (3-10 mg/kg) intraduodenally or intragastrically, the pressor response to AII (250 ng/kg, i.v.) was inhibited in a dose-dependent manner. For three hours, a notable suppression of the pressor response to AII was noted at 10 mg/kg, i.d.[1].
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| References |
| Molecular Formula |
C23H24N2O4S
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|---|---|
| Molecular Weight |
424.51
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| Exact Mass |
424.15
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| Elemental Analysis |
C, 65.07; H, 5.70; N, 6.60; O, 15.08; S, 7.55
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| CAS # |
133040-01-4
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| Related CAS # |
Eprosartan mesylate; 144143-96-4; Eprosartan-d3; 1185243-70-2
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| Appearance |
Solid powder
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| SMILES |
CCCCC1=NC=C(N1CC2=CC=C(C=C2)C(=O)O)/C=C(\CC3=CC=CS3)/C(=O)O
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| InChi Key |
OROAFUQRIXKEMV-LDADJPATSA-N
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| InChi Code |
InChI=1S/C23H24N2O4S/c1-2-3-6-21-24-14-19(12-18(23(28)29)13-20-5-4-11-30-20)25(21)15-16-7-9-17(10-8-16)22(26)27/h4-5,7-12,14H,2-3,6,13,15H2,1H3,(H,26,27)(H,28,29)/b18-12+
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| Chemical Name |
4-[[2-butyl-5-[(E)-2-carboxy-3-thiophen-2-ylprop-1-enyl]imidazol-1-yl]methyl]benzoic acid
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| Synonyms |
Regulaten; Futuran; Navixen; Teveten; SKF-108566; SKF108566; Teveten; SKF 108566; SK and F 108566
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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: ~125 mg/mL (~294.5 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.90 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 20.8 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: ≥ 2.08 mg/mL (4.90 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 20.8 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: ≥ 2.08 mg/mL (4.90 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 | 2.3557 mL | 11.7783 mL | 23.5566 mL | |
| 5 mM | 0.4711 mL | 2.3557 mL | 4.7113 mL | |
| 10 mM | 0.2356 mL | 1.1778 mL | 2.3557 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01087749 | Completed | Drug: Propranolol Drug: Eprosartan |
Kidney Disease | University of California, San Francisco |
March 2010 | Phase 1 |
| NCT00160160 | Completed | Drug: eprosartan/HCTZ | Hypertension Type 2 Diabetes |
Solvay Pharmaceuticals | October 2004 | Not Applicable |
| NCT00438945 | Completed | Drug: Eprosartan | Essential Hypertension | Regional Hospital Holstebro | January 2007 | Phase 4 |
| NCT00409903 | Completed | Drug: Eprosartan | Healthy | Regional Hospital Holstebro | November 2006 | Phase 4 |
| NCT01631227 | Completed | Drug: Eprosartan Drug: Placebo Eprosartan |
Essential Hypertension | Abbott | June 2012 | Phase 3 |
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