Betamipron
Based on 1 Customer Validation
Betamipron (N-benzoyl-β-alanine) is a carbapenem β-lactam antibiotic with antibacterial activity against most Gram-positive and Gram-negative aerobic and anaerobic bacteria. Betamipron can target and inhibit renal organic anion transporters, alleviate renal injury caused by Cisplatin (HY-17394), without interfering with the biological activity of cisplatin. Betamipron is often used in combination with panipenem, which can attenuate the renal effects induced by panipenem and slightly promote the proliferation of Clostridium difficile in the cecum. Betamipron can be used in studies related to renal injury and bacterial infection.
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- Purity : 98.69%
- CAS No.: 3440-28-6
- 화학식: C10H11NO3
- 분자량:193.20
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
[1]|
β-lactam |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
6 μM
Compound: Betamipron
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TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells
TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells
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[PMID: 10991954] |
| S2 | IC50 |
39 μM
Compound: Betamipron
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TP_TRANSPORTER: inhibition of PHA uptake (PHA: 5uM) in hOAT1-expressing S2 cells
TP_TRANSPORTER: inhibition of PHA uptake (PHA: 5uM) in hOAT1-expressing S2 cells
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[PMID: 14978359] |
| S2 | IC50 |
47.5 μM
Compound: Betamipron
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TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in rOAT3-expressing S2 cells
TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in rOAT3-expressing S2 cells
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[PMID: 14978359] |
| S2 | IC50 |
483 μM
Compound: Betamipron
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TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT4-expressing S2 cells
TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT4-expressing S2 cells
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[PMID: 14978359] |
| S2 | IC50 |
9.92 μM
Compound: Betamipron
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TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT3-expressing S2 cells
TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT3-expressing S2 cells
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[PMID: 14978359] |
In Vitro
Betamipron (1:1 ratio with panipenem) inhibits renal dehydropeptidase-I and kidney anion transport to reduce panipenem-associated kidney toxicity and prevent panipenem hydrolysis by renal DHP-I[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Betamipron (250 mg/kg; i.p.; single dose) significantly suppresses Cisplatin (HY-17394)-induced nephrotoxicity in male Wistar rats; significantly reduced Cisplatin-induced weight loss in male ddY mice and decreased serum BUN levels; and did not alter the antileukemic efficacy of cisplatin in male BDF1 mice carrying P388 leukemia[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICI strain (male, 5 weeks old, 20g)[1]
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Dosage:100 mg/kg (as part of a 1:1 panipenem/betamipron formulation)
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Administration:s.c.; once daily; 5 days
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Result:Reduced Clostridium difficile counts in cecal contents to below 102 CFU/g in all 5 mice 1 day after the end of dosing.
Resulted in *Clostridium difficile* counts of 102 CFU/g in 1 mouse and 103 CFU/g in 4 mice 7 days after the end of dosing.
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Animal Model:Wistar (male, 235-365 g, cisplatin-induced nephrotoxicity model)
ddY (male, 25-32 g, cisplatin-induced nephrotoxicity model)
BDF1 (male, 5 weeks old, 21-24.5 g, P388 leukemia model)
[2] -
Dosage:250 mg/kg
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Administration:i.p.; single dose (1 hour after cisplatin)
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Result:Blocked cisplatin-induced weight loss, with a 9.37% weight gain versus a 10.8% loss in the cisplatin group. Studies were conducted on male Wistar rats with cisplatin-induced nephrotoxicity.
Decreased serum BUN and creatinine to normal levels, which remained high in rats given cisplatin alone. Studies were conducted on male Wistar rats with cisplatin-induced nephrotoxicity.
Recovered cisplatin-altered water intake, urine volume and pH. Studies were conducted on male Wistar rats with cisplatin-induced nephrotoxicity.
Normalized abnormal urinary biochemical indicators caused by cisplatin. Studies were conducted on male Wistar rats with cisplatin-induced nephrotoxicity.
Mitigated cisplatin-triggered weight loss obviously compared with the combination of cisplatin and alkaline solution. Studies were conducted on male ddY mice with cisplatin-induced nephrotoxicity.
Reduced elevated serum BUN in mice receiving cisplatin plus alkaline solution. Studies were conducted on male ddY mice with cisplatin-induced nephrotoxicity.
Achieved similar survival benefits as cisplatin combined with alkaline solution. Studies were conducted on male BDF1 mice with P388 leukemia.
Extended survival in all cisplatin-treated mice compared with controls. Studies were conducted on male BDF1 mice with P388 leukemia.
Chemical Information
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CAS No. 3440-28-6
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Appearance Solid
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분자량 193.20
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화학식 C10H11NO3
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Color White to off-white
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SMILES
O=C(O)CCNC(C1=CC=CC=C1)=O
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Synonyms
N-Benzoyl-β-alanine
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
In Vitro:
DMSO : 100 mg/mL (517.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (12.94 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (12.94 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 5.1760 mL | 25.8799 mL | 51.7598 mL | 129.3996 mL |
| 5 mM | 1.0352 mL | 5.1760 mL | 10.3520 mL | 25.8799 mL | |
| 10 mM | 0.5176 mL | 2.5880 mL | 5.1760 mL | 12.9400 mL | |
| 15 mM | 0.3451 mL | 1.7253 mL | 3.4507 mL | 8.6266 mL | |
| 20 mM | 0.2588 mL | 1.2940 mL | 2.5880 mL | 6.4700 mL | |
| 25 mM | 0.2070 mL | 1.0352 mL | 2.0704 mL | 5.1760 mL | |
| 30 mM | 0.1725 mL | 0.8627 mL | 1.7253 mL | 4.3133 mL | |
| 40 mM | 0.1294 mL | 0.6470 mL | 1.2940 mL | 3.2350 mL | |
| 50 mM | 0.1035 mL | 0.5176 mL | 1.0352 mL | 2.5880 mL | |
| 60 mM | 0.0863 mL | 0.4313 mL | 0.8627 mL | 2.1567 mL | |
| 80 mM | 0.0647 mL | 0.3235 mL | 0.6470 mL | 1.6175 mL | |
| 100 mM | 0.0518 mL | 0.2588 mL | 0.5176 mL | 1.2940 mL |
Betamipron Related Classifications
HY-B1127 Related Classifications
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