| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
angiotensin II receptor[1]
Angiotensin II type 1 receptor (AT1R). |
|---|---|
| ln Vitro |
The active metabolite (Azilsartan) exhibits high affinity and selectivity for the AT1 receptor, blocking the binding of angiotensin II. This blockade inhibits the vasoconstricting and aldosterone-secreting effects of angiotensin II, leading to a reduction in blood pressure.
|
| Enzyme Assay |
A radioligand binding assay is standard practice. Membranes from CHO cells expressing the human AT1 receptor are incubated with 125I-labeled [Sar1, Ile8]-angiotensin II in the presence of varying concentrations of the active metabolite (Azilsartan). The Ki value for AT1 receptor antagonism is calculated.
|
| Cell Assay |
HEK293 cells expressing the AT1 receptor are treated with Angiotensin II in the presence of the active metabolite (Azilsartan). Intracellular calcium mobilization (a Gq-mediated event) is measured using a fluorescent indicator. The IC50 for blocking the angiotensin II-induced calcium signal is determined.
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| Animal Protocol |
Spontaneously hypertensive rats (SHR) are orally administered Azilsartan mopivabil (e.g., 0.1-3 mg/kg). Blood pressure is measured via radiotelemetry or tail-cuff plethysmography. Efficacy is demonstrated by a dose-dependent reduction in mean arterial pressure over a 24-hour period.
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| ADME/Pharmacokinetics |
Following oral administration, the mopivabil ester is rapidly hydrolyzed to the active parent compound, Azilsartan. Azilsartan has a relatively long terminal half-life (approx. 11-12 hours) and is highly bound to plasma proteins (mainly albumin). It is primarily excreted unchanged in feces.
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| Toxicity/Toxicokinetics |
Azilsartan mopivabil is a prodrug that is well-tolerated. Common adverse effects observed in clinical studies include dizziness, headache, and mild gastrointestinal disturbances. Serious toxicities are rare but may include angioedema or renal impairment.
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| References | |
| Additional Infomation |
Azilsartan Mopivabil is a small molecule drug. The International Nonproprietary Name (INN) stem "-sartan" in its name indicates that azilsartan mopivabil is an angiotensin II receptor antagonist, belonging to the non-peptide antihypertensive class. The monoisotopic molecular weight of azilsartan mopivabil is 676.25 Da.
See also: Azilsartan (containing the active moiety). Azilsartan mopivabil (Edarbi) is an FDA-approved angiotensin II receptor blocker (ARB) used for the treatment of hypertension. The mopivabil ester is a prodrug modification designed to improve oral bioavailability. It offers a once-daily dosing regimen. |
| Molecular Formula |
C38H36N4O8
|
|---|---|
| Molecular Weight |
676.714449882507
|
| Exact Mass |
676.253
|
| CAS # |
2271428-31-8
|
| PubChem CID |
162623520
|
| Appearance |
White to off-white solid powder
|
| LogP |
7.3
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
50
|
| Complexity |
1220
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O(CC)C1=NC2C=CC=C(C(=O)OCC3C=CC(=C(C=3)OC)OC(C(C)(C)C)=O)C=2N1CC1C=CC(C2=CC=CC=C2C2=NOC(N2)=O)=CC=1
|
| InChi Key |
UIGUEOKVFZHFSB-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C38H36N4O8/c1-6-47-36-39-29-13-9-12-28(34(43)48-22-24-16-19-30(31(20-24)46-5)49-35(44)38(2,3)4)32(29)42(36)21-23-14-17-25(18-15-23)26-10-7-8-11-27(26)33-40-37(45)50-41-33/h7-20H,6,21-22H2,1-5H3,(H,40,41,45)
|
| Chemical Name |
[4-(2,2-dimethylpropanoyloxy)-3-methoxyphenyl]methyl 2-ethoxy-3-[[4-[2-(5-oxo-4H-1,2,4-oxadiazol-3-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 95 mg/mL (140.39 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4777 mL | 7.3887 mL | 14.7774 mL | |
| 5 mM | 0.2955 mL | 1.4777 mL | 2.9555 mL | |
| 10 mM | 0.1478 mL | 0.7389 mL | 1.4777 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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