| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
RNPA1000 targets RnpA, a dual-function enzyme in Staphylococcus aureus that participates in two essential cellular processes: RNA degradation and tRNA maturation. RnpA is a promising novel antimicrobial target. RNPA1000 inhibits RnpA-mediated cellular RNA degradation and tRNA maturation. By inhibiting these essential functions, RNPA1000 disrupts bacterial growth and survival.
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| 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].
In vitro, RNPA1000 is a potent inhibitor of RnpA. It inhibits tRNA maturation with an IC50 of 175 μM. The compound exhibits antibacterial efficacy against Gram-positive bacteria. It displays specificity for RnpA, as it does not significantly affect the in vitro activities of unrelated bacterial or eukaryotic ribonucleases. RNPA1000 is a valuable tool for studying RnpA function and for developing new antimicrobial agents. |
| ln Vivo |
In vivo activity data for RNPA1000 is limited, as the compound is primarily used as a research tool in in vitro studies. However, it is an attractive antimicrobial development candidate. The compound has been included in studies alongside vancomycin for preclinical development. Its potential for in vivo applications is supported by its specificity for RnpA and its lack of measurable human cytotoxicity.
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| Enzyme Assay |
In vitro enzyme assays for RNPA1000 measure its inhibition of RnpA-mediated RNA degradation and tRNA maturation. The enzyme is incubated with its RNA substrates in the presence of varying concentrations of the compound. The activity of RnpA is measured by quantifying the degradation of RNA or the processing of tRNA precursors. The IC50 is determined from dose-response curves.
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| Cell Assay |
In vitro cell-based assays for RNPA1000 are conducted using Staphylococcus aureus cultures. Bacteria are treated with the compound at various concentrations, and bacterial growth is monitored. The minimum inhibitory concentration (MIC) is determined. These assays confirm the compound's antibacterial activity and its specificity for RnpA.
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| Animal Protocol |
In vivo animal experiments for RNPA1000 are not extensively described in the available literature. As a research compound, its use in vivo would be determined by the specific research question being addressed. A typical protocol for studying an antimicrobial compound would involve its administration to animal models of bacterial infection. However, specific protocols for RNPA1000 are not detailed.
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| ADME/Pharmacokinetics |
RNPA1000 has a molecular weight of 464.31 g/mol and a molecular formula of C23H18BrN3O3. It is a white solid with a purity of ≥98%. It is soluble in DMSO. For storage, it is recommended to keep the powder at -20°C. The compound has a shelf life of 2 years from the QC date when stored properly.
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| Toxicity/Toxicokinetics |
RNPA1000 exhibits minimal toxicity to human cells. It displays specificity for RnpA and does not significantly affect the in vitro activities of unrelated bacterial or eukaryotic ribonucleases. As with all research chemicals, standard laboratory safety precautions should be followed when handling RNPA1000. Its use is limited to research applications.
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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. |
| Additional Infomation |
RNPA1000 is a research compound and is not approved for any clinical or therapeutic use. It is a potent RnpA inhibitor and an attractive antimicrobial development candidate. It has been studied as a potential therapeutic agent for Staphylococcus aureus infections. Its mechanism of action involves inhibiting RnpA-mediated RNA degradation and tRNA maturation. RNPA1000 is a valuable research tool for studying RnpA function and for developing new antimicrobial agents.
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| 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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