| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 5g |
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| Other Sizes |
| Targets |
Betamipron targets renal organic anion transporters and dipeptidases. By inhibiting the uptake of panipenem into renal tubular cells, it reduces the nephrotoxicity of the antibiotic. The compound competitively inhibits the renal tubular organic anion transporter system, which is responsible for the active uptake of nephrotoxic compounds, particularly certain antibiotics like panipenem. By blocking this transport pathway, Betamipron effectively decreases the renal accumulation of panipenem and prevents kidney damage. The compound is also a substrate for these transporters. Betamipron's mechanism of action is based on its ability to compete with panipenem for binding to renal organic anion transporters, thereby reducing the intracellular concentration of the antibiotic in renal tubular cells and mitigating its nephrotoxic effects.
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| ln Vitro |
In vitro, Betamipron has been shown to inhibit the uptake of panipenem into renal tubular cells. It also inhibits dipeptidase activity. The compound's ability to inhibit renal organic anion transporters can be assessed using cell culture models of renal proximal tubule cells. In these models, the uptake of radiolabeled or fluorescently labeled panipenem is measured in the presence and absence of Betamipron. The compound's inhibitory effect on dipeptidase activity can be assessed using enzyme activity assays with appropriate substrates. The compound's cytotoxicity in renal cell models can also be evaluated.
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| ln Vivo |
In vivo, Betamipron is used in combination with panipenem to reduce nephrotoxicity. It is administered intravenously as a fixed-combination product with panipenem at a 1:1 weight ratio. By inhibiting the renal uptake of panipenem, Betamipron helps prevent kidney damage, making this combination safer for patients requiring potent antibacterial therapy. The compound's nephroprotective effects have been demonstrated in various preclinical and clinical studies. Betamipron does not significantly affect the antibacterial activity of panipenem, as its action is limited to the renal tubules.
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| Enzyme Assay |
For non-cellular enzyme assays, Betamipron can be tested for inhibition of dipeptidase activity using standard enzyme activity assays. The enzyme is incubated with varying concentrations of the compound, and the hydrolysis of dipeptide substrates is measured. The compound's interaction with renal organic anion transporters can be studied using membrane preparations or purified transporter proteins in reconstituted systems. The compound's binding affinity to transporters can be assessed using radioligand binding assays or surface plasmon resonance.
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| Cell Assay |
For in vitro cell-based assays, renal proximal tubule cells are cultured and treated with Betamipron. The uptake of panipenem is measured in the presence and absence of the compound. Cell viability and cytotoxicity are assessed using MTT or similar assays. The compound's effects on transporter expression and function can be evaluated using molecular biology techniques. The compound's protective effects against panipenem-induced cytotoxicity can be assessed by co-treatment with panipenem and Betamipron.
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| Animal Protocol |
For in vivo animal studies, Betamipron is administered with panipenem to animal models. The compound is typically administered intravenously. Renal function is assessed by measuring serum creatinine, blood urea nitrogen, and other markers of kidney function. Histological examination of kidney tissues is performed to assess renal damage. The pharmacokinetic and pharmacodynamic properties of the combination are evaluated. The compound's nephroprotective effects are compared to panipenem alone.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Betamipron include a molecular weight of 193.2 and a molecular formula of C₁₀H₁₁NO₃. The compound is soluble in DMSO at 37 mg/mL (191.51 mM) and in ethanol at 37 mg/mL (191.51 mM), but is insoluble in water. The compound should be stored lyophilized at -20°C, kept desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, it should be stored at -20°C and used within 3 months to prevent loss of potency. The compound should be aliquoted to avoid multiple freeze/thaw cycles.
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| Toxicity/Toxicokinetics |
Betamipron is generally well-tolerated. As a nephroprotective agent, its safety profile is favorable. The compound is used clinically in combination with panipenem and has been shown to reduce the incidence of nephrotoxicity associated with carbapenem antibiotics. The compound is intended for research use only and is not for human use in research settings.
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| Additional Infomation |
Betamipron is an organic nitrogen and organic oxygen compound whose function is related to β-amino acids.
Betamipron (CS-443) is a nephroprotective agent used in combination with panipenem to prevent nephrotoxicity. It competitively inhibits the renal tubular organic anion transporter system, reducing the uptake of panipenem into renal proximal tubule cells. The compound is clinically administered as a 1:1 fixed-combination product with panipenem (Carbenin®). Betamipron is an N-benzoyl-β-alanine derivative. It is not currently approved for clinical use as a standalone agent and is available only for research purposes. |
| Molecular Formula |
C10H11NO3
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|---|---|
| Molecular Weight |
193.1992
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| Exact Mass |
193.074
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| CAS # |
3440-28-6
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| PubChem CID |
71651
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| Appearance |
White to off-white solid powder
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| Density |
1.227 g/cm3
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| Boiling Point |
469.2ºC at 760 mmHg
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| Melting Point |
132 °C
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| Flash Point |
237.6ºC
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| Index of Refraction |
1.557
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| LogP |
1.282
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
14
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| Complexity |
209
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CWXYHOHYCJXYFQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H11NO3/c12-9(13)6-7-11-10(14)8-4-2-1-3-5-8/h1-5H,6-7H2,(H,11,14)(H,12,13)
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| Chemical Name |
3-benzamidopropanoic acid
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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 (~517.60 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.94 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 (12.94 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 (12.94 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 | 5.1760 mL | 25.8799 mL | 51.7598 mL | |
| 5 mM | 1.0352 mL | 5.1760 mL | 10.3520 mL | |
| 10 mM | 0.5176 mL | 2.5880 mL | 5.1760 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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