| Size | Price | Stock | Qty |
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| 1mg |
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| 100mg | |||
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| Targets |
Bacterial RNA polymerase (RNAP), specifically the enzyme's active site. Pseudouridimycin is a selective bacterial RNA polymerase inhibitor that competes with UTP for access to the RNAP active site, thereby blocking transcription initiation and bacterial growth. The compound does not inhibit mammalian RNA polymerases, making it a highly selective antibacterial agent. Its unique mechanism of action differs from traditional antibiotics, offering potential against drug-resistant strains.
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| ln Vitro |
In vitro, Pseudouridimycin exhibits potent antibacterial activity against a wide range of Gram-positive and Gram-negative bacteria. It potently inhibits bacterial RNAP with an IC50 of 0.1 microM and inhibits bacterial growth with IC50 values ranging from 2 to 16 microM. The compound functions by binding to the RNAP active site and preventing the formation of the transcription initiation complex. Its unique chemical structure and mechanism of action make it a promising candidate for treating bacterial infections, particularly those caused by multidrug-resistant pathogens.
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| ln Vivo |
In vivo, Pseudouridimycin has demonstrated efficacy in animal models of infection. In a mouse Streptococcus pyogenes peritonitis model, the compound cleared infection at doses of 3.2-50 mg/kg administered intravenously, with an ED50 of 9 mg/kg. The compound showed antibacterial activity in vivo in female ICR mice following intraperitoneal injection. Pseudouridimycin inhibits bacterial growth in culture and has shown in vivo efficacy in animal models of infection, making it a promising candidate for further development as a novel antibiotic.
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| Enzyme Assay |
In vitro RNA polymerase inhibition assays for Pseudouridimycin measure inhibition of bacterial RNAP enzymatic activity. The assay uses recombinant bacterial RNA polymerase (core or holoenzyme) and a DNA template with a fluorescent or radiolabeled nucleotide substrate. The compound is serially diluted in assay buffer and pre-incubated with the enzyme for 15-30 minutes. The reaction is initiated by adding DNA template and nucleotides, and after incubation at 37degC, RNA synthesis is measured by fluorescence, scintillation counting, or gel electrophoresis. IC50 values are calculated from dose-response curves.
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| Cell Assay |
In vitro antibacterial susceptibility assays for Pseudouridimycin are performed using standard broth microdilution methods following CLSI guidelines. Bacterial strains (Gram-positive and Gram-negative) are cultured in appropriate media to mid-log phase. Pseudouridimycin is serially diluted in 96-well plates, and bacterial suspensions are added to achieve a final concentration of approximately 5×10⁵ CFU/mL. Plates are incubated at 37degC for 18-24 hours. The minimum inhibitory concentration (MIC) is determined as the lowest concentration that inhibits visible bacterial growth. IC50 values for bacterial growth inhibition are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for Pseudouridimycin are conducted in mouse models of bacterial infection. In the Streptococcus pyogenes peritonitis model, female ICR mice (23-25 g) are infected intraperitoneally with 4×103 CFU of S. pyogenes in 0.5 mL saline supplemented with 1% peptone. Pseudouridimycin is administered intravenously at doses of 3.2-50 mg/kg, 10 minutes after infection and again 6 hours after infection. Survival and bacterial clearance are monitored. The ED50 is calculated as 9 mg/kg.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Pseudouridimycin have been characterized in preclinical studies. With a molecular weight of 486.44 and a molecular formula of C17H26N8O9, the compound is soluble in DMSO. It is typically stored as a powder at -20degC for up to 3 years or in solution at -80degC for up to 1 year. The compound has a predicted density of 1.91+/-0.1 g/cm3. Standard pharmacokinetic parameters (clearance, volume of distribution, half-life, bioavailability) can be determined following intravenous and oral administration in preclinical species.
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| Toxicity/Toxicokinetics |
Pseudouridimycin is intended for research use only and is not for human therapeutic use. Standard safety precautions for handling chemical compounds apply. The compound is not approved for clinical use. Preclinical toxicity studies would be required before clinical development.
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| References | |
| Additional Infomation |
Pseudouridimycin is a glutamine derivative. It has been reported that pseudouridinemycin is found in both Streptomyces and Streptomyces albopictus, and relevant data are available for reference.
Pseudouridimycin is a research-grade C-nucleoside analogue antibiotic that selectively inhibits bacterial RNA polymerase. Its synonyms include PUM and (1S)-1,4-Anhydro-5-[(N-carbamimidoylglycyl-N2-hydroxy-L-glutaminyl)amino]-5-deoxy-1-(2,4-dioxo-1,2,3,4-tetrahydro-5-pyrimidinyl)-D-ribitol. Purity is typically ≥95%. The compound is effective against both Gram-negative and Gram-positive bacteria and is derived from Streptomyces species. Its unique mode of action targeting bacterial RNAP makes it a promising candidate for treating multidrug-resistant infections. Not approved for clinical use. |
| Molecular Formula |
C17H26N8O9
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|---|---|
| Molecular Weight |
486.436542987823
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| Exact Mass |
486.182
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| CAS # |
1566586-52-4
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| PubChem CID |
72792467
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
-5.9
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
34
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| Complexity |
903
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| Defined Atom Stereocenter Count |
5
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| SMILES |
O1[C@@H](C2=CNC(NC2=O)=O)[C@@H]([C@@H]([C@H]1CNC([C@H](CCC(N)=O)N(C(C/N=C(\N)/N)=O)O)=O)O)O
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| InChi Key |
XDEYHXABZOKKDZ-YFKLLHAASA-N
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| InChi Code |
InChI=1S/C17H26N8O9/c18-9(26)2-1-7(25(33)10(27)5-22-16(19)20)15(31)21-4-8-11(28)12(29)13(34-8)6-3-23-17(32)24-14(6)30/h3,7-8,11-13,28-29,33H,1-2,4-5H2,(H2,18,26)(H,21,31)(H4,19,20,22)(H2,23,24,30,32)/t7-,8+,11+,12+,13-/m0/s1
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| Chemical Name |
(2S)-2-[[2-(diaminomethylideneamino)acetyl]-hydroxyamino]-N-[[(2R,3S,4R,5S)-5-(2,4-dioxo-1H-pyrimidin-5-yl)-3,4-dihydroxyoxolan-2-yl]methyl]pentanediamide
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0558 mL | 10.2788 mL | 20.5575 mL | |
| 5 mM | 0.4112 mL | 2.0558 mL | 4.1115 mL | |
| 10 mM | 0.2056 mL | 1.0279 mL | 2.0558 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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