Cilastatin-15N,d3
Based on 1 Customer Validation
Cilastatin-15N,d3 is a 15N-labeled and deuterium labeled Cilastatin. Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct.
For research use only. We do not sell to patients.
- Purity: 99.71%
- CAS No.: 2738376-83-3
- Formula: C16H23D3N15NO5S
- Molecular Weight:362.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All Antibiotic Isoforms
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Biological Activity
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β-lactam |
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 2738376-83-3
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Unlabeled Cas 82009-34-5
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Appearance Solid
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Molecular Weight 362.46
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Formula C16H23D3N15NO5S
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Color White to off-white
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SMILES
O=C(O)/C(NC([C@@H]1C(C)(C)C1)=O)=C/CCCCSC([2H])([2H])C([15NH2])([2H])C(O)=O
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Synonyms
MK0791-15N,d3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (275.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
1 M NaOH : 100 mg/mL (275.89 mM; ultrasonic and adjust pH to 12 with NaOH)
H2O : 12.5 mg/mL (34.49 mM; ultrasonic and warming and heat to 60°C)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-223. [Content Brief]
[2]. The renal membrane dipeptidase (dehydropeptidase I) inhibitor, cilastatin, inhibits the bacterialmetallo-beta-lactamase enzyme CphA. Antimicrob Agents Chemother. 1995 Jul;39(7):1629-31. [Content Brief]
[3]. Blanca Humanes, et al. Protective Effects of Cilastatin Against Vancomycin-Induced Nephrotoxicity. Biomed Res Int. 2015;2015:704382. [Content Brief]
[4]. P J Petersen, et al. In Vitro and in Vivo Activities of LJC10,627, a New Carbapenem With Stability to Dehydropeptidase I. Antimicrob Agents Chemother. 1991 Jan;35(1):203-7. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO / 1 M NaOH | 1 mM | 2.7589 mL | 13.7946 mL | 27.5893 mL | 68.9731 mL |
| 5 mM | 0.5518 mL | 2.7589 mL | 5.5179 mL | 13.7946 mL | |
| 10 mM | 0.2759 mL | 1.3795 mL | 2.7589 mL | 6.8973 mL | |
| 15 mM | 0.1839 mL | 0.9196 mL | 1.8393 mL | 4.5982 mL | |
| 20 mM | 0.1379 mL | 0.6897 mL | 1.3795 mL | 3.4487 mL | |
| 25 mM | 0.1104 mL | 0.5518 mL | 1.1036 mL | 2.7589 mL | |
| 30 mM | 0.0920 mL | 0.4598 mL | 0.9196 mL | 2.2991 mL | |
| DMSO / 1 M NaOH | 40 mM | 0.0690 mL | 0.3449 mL | 0.6897 mL | 1.7243 mL |
| 50 mM | 0.0552 mL | 0.2759 mL | 0.5518 mL | 1.3795 mL | |
| 60 mM | 0.0460 mL | 0.2299 mL | 0.4598 mL | 1.1496 mL | |
| 80 mM | 0.0345 mL | 0.1724 mL | 0.3449 mL | 0.8622 mL | |
| 100 mM | 0.0276 mL | 0.1379 mL | 0.2759 mL | 0.6897 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.