| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| 10mg | |||
| Other Sizes |
| Targets |
The primary target of Arg-AMS is arginyl tRNA synthetase, an enzyme that catalyzes the attachment of arginine to its cognate tRNA during protein synthesis. The compound binds tightly to the A-domains in non-ribosomal peptide synthetases (NRPS) enzymes. Arg-AMS also targets the host protein CD163, which is involved in the entry and replication of porcine blue ear virus (PRRSV) and its highly pathogenic strain HP-PRRSV. By inhibiting arginyl tRNA synthetase and targeting CD163, Arg-AMS disrupts protein synthesis and viral replication, making it a potential therapeutic agent for viral infections and myeloma.
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| ln Vitro |
GrsB's Orn activation domain is inhibited by Arg-AMS, with an IC50 value of 4.6 µM[1].
In vitro, Arg-AMS is a potent inhibitor of arginyl tRNA synthetase, displaying tightly bound inhibitory characteristics for the A-domains in non-ribosomal peptide synthetases (NRPS) enzymes. It exhibits antiviral activity by targeting the host protein CD163, which inhibits porcine blue ear virus (PRRSV) and its highly pathogenic strain HP-PRRSV. The compound's inhibitory activity is concentration-dependent, with effects observed at nanomolar concentrations. Arg-AMS is used in research to study the role of arginyl tRNA synthetase in protein synthesis and to investigate the mechanisms of viral replication and the potential for therapeutic intervention. |
| ln Vivo |
In vivo, Arg-AMS has potential applications in studying viral infections and myeloma. Its antiviral activity against PRRSV and HP-PRRSV suggests that it may be effective in animal models of these viral infections. However, in vivo studies are limited, and further research is needed to evaluate its efficacy, pharmacokinetics, and safety in animal models. The compound's ability to target arginyl tRNA synthetase and CD163 makes it a promising candidate for further development as an antiviral and anticancer agent.
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| Enzyme Assay |
The in vitro enzyme inhibition activity of Arg-AMS can be assessed using cell-free assays with recombinant arginyl tRNA synthetase. A typical protocol involves incubating the enzyme with ATP, arginine, tRNA, and Arg-AMS at various concentrations in a reaction buffer. The reaction is carried out at 37degC for a specified period, and the amount of aminoacylated tRNA is measured using a radioactive or fluorescent assay. The IC50 value is determined by plotting the percentage of enzyme activity remaining against the compound concentration. The binding affinity of Arg-AMS to the A-domains of NRPS enzymes can be assessed using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC).
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| Cell Assay |
For in vitro cellular experiments, cells (e.g., PRRSV-permissive cells, myeloma cells) are cultured in appropriate media and treated with Arg-AMS at various concentrations (typically 0.1-100 uM). For antiviral studies, cells are infected with PRRSV or HP-PRRSV and treated with the compound, and viral replication is assessed by measuring viral RNA levels using qRT-PCR or viral titers using plaque assays. For myeloma studies, cell viability is measured after 24-72 hours of treatment using MTT or CCK-8 assays. The duration of treatment varies depending on the experimental design but typically ranges from 24 to 72 hours.
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| Animal Protocol |
In vivo animal experiments with Arg-AMS would typically involve administration via intraperitoneal or intravenous injection in mouse models of PRRSV infection or myeloma. A common dosing regimen would be based on pharmacokinetic studies to determine the optimal dose and route of administration. For antiviral studies, animals are infected with PRRSV or HP-PRRSV, and Arg-AMS is administered either prophylactically or therapeutically. Viral load in blood and tissues is measured at various time points by qRT-PCR. For myeloma studies, tumor-bearing mice are treated with the compound, and tumor growth is monitored by caliper measurements.
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| ADME/Pharmacokinetics |
Arg-AMS has a molecular weight of 502.51 g/mol and a molecular formula of C16H26N10O7S. It is soluble in DMSO and water at 80 mg/mL. For in vivo studies, it can be formulated in 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline at a concentration of 3.3 mg/mL. The compound should be stored at low temperature (-20degC). Further pharmacokinetic studies are needed to determine its absorption, distribution, metabolism, and excretion properties, including oral bioavailability, half-life, and tissue distribution.
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| Toxicity/Toxicokinetics |
The toxicity profile of Arg-AMS has not been extensively characterized. As an inhibitor of arginyl tRNA synthetase, which is essential for protein synthesis, the compound may have potential toxicity to rapidly dividing cells. However, its selectivity for the viral target CD163 may contribute to a favorable safety profile. In vitro cytotoxicity studies would be needed to assess its effects on mammalian cell lines. In vivo toxicity studies in animal models would also be required to determine its safety profile. The compound should be handled with standard laboratory precautions and is intended for research use only.
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| References | |
| Additional Infomation |
Arg-AMS (compound 24) is a potent nanomolar inhibitor of arginyl tRNA synthetase. It displays tightly bound inhibitory characteristics for the A-domains in non-ribosomal peptide synthetases (NRPS) enzymes. Arg-AMS has antiviral activity and targets the host protein CD163 to inhibit porcine blue ear virus (PRRSV) and its highly pathogenic strain HP-PRRSV. The compound can be used to study viral infections and myeloma. Arg-AMS has a molecular weight of 502.51 g/mol and a molecular formula of C16H26N10O7S. It is available as a research compound and is not approved for clinical use.
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| Molecular Formula |
C16H26N10O7S
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| Molecular Weight |
502.505440235138
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| Exact Mass |
502.17
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| CAS # |
301351-95-1
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| PubChem CID |
9983529
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| Appearance |
White to off-white solid powder
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| LogP |
-4.5
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
34
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| Complexity |
839
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| Defined Atom Stereocenter Count |
5
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| SMILES |
S(NC([C@H](CCC/N=C(\N)/N)N)=O)(=O)(=O)OC[C@@H]1[C@H]([C@H]([C@H](N2C=NC3C(N)=NC=NC2=3)O1)O)O
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| InChi Key |
BPKLMCNLHSJSEL-JVEUSOJLSA-N
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| InChi Code |
InChI=1S/C16H26N10O7S/c17-7(2-1-3-21-16(19)20)14(29)25-34(30,31)32-4-8-10(27)11(28)15(33-8)26-6-24-9-12(18)22-5-23-13(9)26/h5-8,10-11,15,27-28H,1-4,17H2,(H,25,29)(H2,18,22,23)(H4,19,20,21)/t7-,8+,10+,11+,15+/m0/s1
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| Chemical Name |
[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl N-[(2S)-2-amino-5-(diaminomethylideneamino)pentanoyl]sulfamate
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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 : ≥ 100 mg/mL (~199.00 mM)
H2O : ~100 mg/mL (~199.00 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.98 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 (4.98 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 (4.98 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 | 1.9900 mL | 9.9501 mL | 19.9001 mL | |
| 5 mM | 0.3980 mL | 1.9900 mL | 3.9800 mL | |
| 10 mM | 0.1990 mL | 0.9950 mL | 1.9900 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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