| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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Purity: ≥98%
RNPA1000 is a novel and potent inhibitor of growth of Staphylococcus aureus. It is a antimicrobial agent acting as a RNase inhibitor.
| ln Vitro |
RNPA1000 exhibits minimal toxicity to human cells and antibacterial efficacy against Gram-positive bacteria [2]. Staphylococcus aureus mRNA growth and turnover are restricted by RNPA1000. Along with its antimicrobial activity against biofilm-associated Staphylococcus aureus, RNPA1000 also inhibits the growth of other significant Gram-positive bacterial pathogens and guards against S. aureus pathology in animal infection models [3]. Commercially available E. Coli RNase HI, RNase A, RNase I, and in-house purified S. aureus RNase J1 are not affected by RNPA1000 (IC50= 100-125 µM) at any tested concentration (0-750 µM). However, E. Coli RNase III activity (IC50= 500-750 µM) is modestly inhibited[3].
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| References |
[1]. Eidem TM, et al. Drug-eluting cements for hard tissue repair: a comparative study using vancomycin and RNPA1000 to inhibit growth of Staphylococcus aureus. J Biomater Appl. 2014 Apr;28(8):1235-46.
[2]. Eidem TM, et al. Small-molecule inhibitors of Staphylococcus aureus RnpA-mediated RNA turnover and tRNA processing. Antimicrob Agents Chemother. 2015 Apr;59(4):2016-28. [3]. Patrick D Olson, et al. Small molecule inhibitors of Staphylococcus aureus RnpA alter cellular mRNA turnover, exhibit antimicrobial activity, and attenuate pathogenesis. PLoS Pathog. 2011 Feb 10;7(2):e1001287. |
| Molecular Formula |
C23H18BRN3O3
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|---|---|
| Molecular Weight |
464.311324596405
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| Exact Mass |
463.053
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| CAS # |
359600-10-5
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| Related CAS # |
359600-10-5;
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| PubChem CID |
1268985
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| Appearance |
Light yellow to khaki solid powder
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| LogP |
5.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
723
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=C(N1C2=CC=C(C=C2)C(=O)O)C)/C=C(\C#N)/C(=O)NC3=CC(=CC=C3)Br
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| InChi Key |
WQCMDUBFZYCGMI-WOJGMQOQSA-N
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| InChi Code |
InChI=1S/C23H18BrN3O3/c1-14-10-17(15(2)27(14)21-8-6-16(7-9-21)23(29)30)11-18(13-25)22(28)26-20-5-3-4-19(24)12-20/h3-12H,1-2H3,(H,26,28)(H,29,30)/b18-11+ SMILES
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| Chemical Name |
4-[3-[3-[(3-Bromophenyl)amino]-2-cyano-3-oxo-1-propen-1-yl]-2,5-dimethyl-1H-pyrrol-1-yl]-benzoic acid InChi Key
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| Synonyms |
RNPA1000 RNPA-1000 RNPA 1000
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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 : ~50 mg/mL (~107.69 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.38 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 (5.38 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 (5.38 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 | 2.1537 mL | 10.7687 mL | 21.5373 mL | |
| 5 mM | 0.4307 mL | 2.1537 mL | 4.3075 mL | |
| 10 mM | 0.2154 mL | 1.0769 mL | 2.1537 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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