| Size | Price | |
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| 1mg | ||
| Other Sizes |
| Targets |
Mibenratide specifically targets the adrenergic beta1 receptor, a G protein-coupled receptor (GPCR) that is the primary beta-adrenergic receptor subtype in the heart. By binding to this receptor, it blocks the actions of endogenous catecholamines like norepinephrine and epinephrine, thereby reducing sympathetic stimulation of the heart.
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| ln Vitro |
Mibenratide is a cyclic peptide with the sequence Cyclo(Ala-Arg-Arg-Cys-Tyr-Asn-Asp-Pro-Lys-Cys-Ser-Asp-Phe-Val-Gln-Ala-Asp-Glu). It is a potent and selective antagonist of the beta-1 adrenergic receptor. It has a high binding affinity for this receptor, which is a key target for treating cardiac dysfunction. As a cyclic peptide, it is more stable to enzymatic degradation than its linear counterpart.
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| ln Vivo |
Not available. As a preclinical compound, its in vivo activity is currently under investigation. It is expected to decrease heart rate, reduce myocardial oxygen demand, and improve cardiac function in heart failure models. No quantitative in vivo data is available in the provided literature.
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| Enzyme Assay |
Not available. A standard radioligand binding assay for beta1 adrenergic receptors would involve using a membrane preparation from cells (e.g., HEK293) overexpressing the human beta1 receptor. The membranes are incubated with a high-affinity radioligand (e.g., [3H]-CGP 12177) and increasing concentrations of Mibenratide TFA. After incubation, the bound radioligand is separated by filtration and measured by liquid scintillation counting to calculate the Ki.
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| Cell Assay |
Not available. A typical functional assay involves the measurement of cAMP accumulation in beta1-expressing cells. Cells are pre-treated with forskolin to elevate cAMP levels, then incubated with the beta1 agonist isoproterenol in the presence or absence of Mibenratide TFA. The amount of cAMP produced is then measured using a competitive immunoassay (ELISA). A reduction in isoproterenol-stimulated cAMP production indicates beta1 antagonist activity.
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| Animal Protocol |
Not available. A typical in vivo protocol for testing a beta1 antagonist would involve administering the compound to anesthetized rats, either intravenously or orally, and monitoring heart rate, blood pressure, and cardiac contractility via a pressure-volume catheter. For a disease model, the compound would be administered daily for several weeks to rats with heart failure induced by aortic banding or myocardial infarction, followed by echocardiography to assess cardiac function.
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| ADME/Pharmacokinetics |
As a cyclic peptide, Mibenratide is more resistant to proteases than linear peptides, giving it a longer half-life. Its molecular weight is 2211.27, and it is likely administered via injection. Its pharmacokinetic properties are not documented for this specific compound but are critical for its development as a therapeutic candidate.
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| Toxicity/Toxicokinetics |
As a beta1 antagonist, the primary potential toxicities are related to the pharmacological effect: excessive bradycardia, hypotension, and exacerbation of heart failure in some cases. No specific toxicology data is provided, but these are well-understood class effects for this mechanism of action. Preclinical toxicity studies would be required for further development.
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| References |
[1]. Shubhda Dev, et al. Molecular docking analysis of natriuretic peptide receptor-c towards the design of potential atrial fibrillation inhibitors. 2320-7418.
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| Additional Infomation |
Mibenratide TFA is a research-grade, preclinical drug candidate for the treatment of heart failure. It is an experimental cyclic peptide. It is not a dietary supplement, nor is it approved for human use. The product is strictly for laboratory research use.
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| Molecular Formula |
C87H129N27O30S2.C2HF3O2
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|---|---|
| Related CAS # |
Mibenratide;1239011-83-6
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| Appearance |
White to off-white solid powder
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| 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.) |
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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