SPR741 acetate (Synonyms: NAB741 acetate) |
| Katalog-Nr.GC38947 |
SPR741-Acetat (NAB741-Acetat) ist ein kationisches Peptid, das von Polymyxin B abgeleitet ist und ein PotenzierungsmolekÜl ist.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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SPR741 acetate (NAB741 acetate) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 acetate increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 acetate inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741 acetate[1][2].
SPR741 potentiates antibiotics that are substrates of the AcrAB-TolC efflux pump in E. coli, effectively circumventing the contribution of this pump to intrinsic antibiotic resistance. The intrinsic resistance of E. coli to certain antibiotics that is mediated by both the outer membrane and the AcrAB-TolC efflux system can be overcome, or circumvented, by combining the antibiotic with SPR741 but that potentiation of intrinsic resistance due primarily to efflux may be limited[1].SPR741 lacks significant antibacterial activity as a stand-alone agent but interacts with the outer membrane of Gram-negative bacteria to increase permeability and thereby improve the accumulation of coadministered antibiotics inside the pathogen[2].
SPR741 has the ability to permeabilize the outer membrane of Gram-negative bacteria, thus sensitizing them to hydrophobic antibiotics. SPR741 has a significantly safety profile of compared to that of polymyxin B, which suffers severe, dose-limiting nephrotoxicity in humans. In multiday rodent and nonhuman primate studies, polymyxin B exhibited nephrotoxicity at a far-lower exposure-normalized dose than SPR741[1].
[1]. Corbett D, et al. Potentiation of Antibiotic Activity by a Novel Cationic Peptide: Potency and Spectrum of Activity of SPR741. Antimicrob Agents Chemother. 2017 Jul 25;61(8). pii: e00200-17. [2]. Eckburg PB, et al. Safety, Tolerability, Pharmacokinetics, and Drug Interaction Potential of SPR741, an Intravenous Potentiator, after Single and Multiple Ascending Doses and When Combined with β-Lactam Antibiotics in Healthy Subjects. Antimicrob Agents Chemother. 2019 Aug 23;63(9). pii: e00892-19.
| Cas No. | SDF | ||
| Überlieferungen | NAB741 acetate | ||
| Canonical SMILES | CC(N[C@@H]([C@H](O)C)C(N[C@H](CO)C(N[C@@H](CCNC([C@](N1)([H])[C@H](O)C)=O)C(N[C@@H](CCN)C(N[C@@H](C(N[C@H](C(N[C@H](C(N[C@@H](CCN)C1=O)=O)CCN)=O)CC(C)C)=O)CC2=CC=CC=C2)=O)=O)=O)=O)=O.CC(O)=O | ||
| Formula | C46H77N13O15 | M.Wt | 1052.18 |
| Löslichkeit | DMSO: 130 mg/mL (123.55 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 950.4 μL | 4.752 mL | 9.5041 mL |
| 5 mM | 190.1 μL | 950.4 μL | 1.9008 mL |
| 10 mM | 95 μL | 475.2 μL | 950.4 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)
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