| 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 |
| Targets |
angiotensin II receptor[1]
Mopivabil targets the angiotensin II receptor (AT1 receptor), a G protein-coupled receptor that mediates the vasoconstrictor and aldosterone-secreting effects of angiotensin II. By acting as an antagonist, Mopivabil blocks angiotensin II binding to the AT1 receptor, thereby inhibiting downstream signaling pathways involved in vasoconstriction, sodium retention, and fibrosis. |
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| ln Vitro |
Not available. Mopivabil is an angiotensin II receptor blocker (antagonist). Specific in vitro activity data, such as binding affinity (IC50, Ki) or inhibition of angiotensin II-induced calcium flux or cell contraction, is not provided in the literature. The compound's activity is inferred from its classification as an ARB.
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| ln Vivo |
Not available. As an ARB, Mopivabil is expected to lower blood pressure, reduce cardiac afterload, and provide organ protection in hypertensive animal models. However, specific in vivo efficacy data (e.g., reduction in mean arterial pressure, inhibition of angiotensin II-induced pressor response) is not provided in the literature.
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| Enzyme Assay |
Standard in vitro binding assays for AT1 receptor antagonism involve using membrane preparations from cells overexpressing the human AT1 receptor (e.g., CHO-AT1 cells). Membranes (10-50 microg protein) are incubated with a radiolabeled angiotensin II analog (e.g., [125I]Sar1-Ile8-angiotensin II, 0.1-1 nM) and varying concentrations of Mopivabil (1 pM-100 microM) in binding buffer (50 mM Tris-HCl, pH 7.4, 5 mM MgCl2, 0.1% BSA) at room temperature for 60-120 minutes. Non-specific binding is determined using 10 microM unlabeled angiotensin II. Bound radioligand is separated by filtration, and radioactivity is measured. Ki values are calculated from competition curves.
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| Cell Assay |
A standard cellular functional assay involves measuring angiotensin II-induced intracellular calcium mobilization in cells expressing AT1 receptors (e.g., HEK293-AT1 cells). Cells are loaded with a calcium-sensitive dye (e.g., Fluo-4 AM) for 30-60 minutes at 37degC. Cells are pre-incubated with varying concentrations of Mopivabil (1 nM-100 microM) for 10-15 minutes, then stimulated with angiotensin II (typically 1-10 nM). The increase in fluorescence is measured using a fluorescence plate reader. The IC50 for inhibition of the calcium response is calculated.
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| Animal Protocol |
For in vivo studies, Mopivabil can be administered to hypertensive animal models (e.g., spontaneously hypertensive rats or angiotensin II-infused mice) by oral gavage (e.g., 1-30 mg/kg) or intraperitoneal injection. Blood pressure is measured by tail-cuff plethysmography or telemetry before and after dosing. Plasma renin activity, aldosterone levels, and urine sodium excretion can be measured to assess RAAS blockade. Efficacy is determined as a dose-dependent reduction in blood pressure.
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| ADME/Pharmacokinetics |
Mopivabil has a molecular formula of C14H20O3 and a molecular weight of 236.31. It is an oily liquid (colorless to light yellow) at room temperature. It is soluble in DMSO (100 mg/mL, ~423 mM) for in vitro studies. For in vivo formulation, it can be dissolved in co-solvent systems such as 10% DMSO, 40% PEG300, 5% Tween-80, 45% saline. Storage at -20degC is recommended.
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| Toxicity/Toxicokinetics |
No specific toxicological data for Mopivabil is available. As an angiotensin II receptor antagonist, its class-related toxicities include hypotension, hyperkalemia, renal impairment (especially in patients with bilateral renal artery stenosis), and teratogenicity (contraindicated in pregnancy). At research doses (1-30 mg/kg in rodents), ARBs are generally well-tolerated with a favorable safety margin.
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| References | |
| Additional Infomation |
Mopivabil is a research-grade angiotensin II receptor antagonist (ARB). ARBs are a well-established class of antihypertensive drugs, but Mopivabil itself is not an approved drug. It is strictly for laboratory research in cardiovascular and renal pathophysiology. This product is not intended for human therapeutic use. Common approved ARBs include losartan, valsartan, and candesartan; Mopivabil is an experimental research tool compound.
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| Molecular Formula |
C14H20O3
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|---|---|
| Molecular Weight |
236.31
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| Exact Mass |
236.141
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| CAS # |
2988562-84-9
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| PubChem CID |
162641739
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| Appearance |
Colorless to light yellow ointment
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
17
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| Complexity |
255
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCC1=CC(=C(C=C1)OC(=O)C(C)(C)C)OC
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| InChi Key |
ZITQYHHKBYAVSF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H20O3/c1-6-10-7-8-11(12(9-10)16-5)17-13(15)14(2,3)4/h7-9H,6H2,1-5H3
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| Chemical Name |
(4-ethyl-2-methoxyphenyl) 2,2-dimethylpropanoate
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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 (~423.17 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.58 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 (10.58 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 (10.58 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 | 4.2317 mL | 21.1586 mL | 42.3173 mL | |
| 5 mM | 0.8463 mL | 4.2317 mL | 8.4635 mL | |
| 10 mM | 0.4232 mL | 2.1159 mL | 4.2317 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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