P-536 exhibits broad-spectrum antiviral activity. In their respective host cells, its CPE50 against adenovirus type 5 is 20 μg/mL, against HSV-1, poliovirus type 1 and encephalocarditis virus is 30 μg/mL, against vaccinia virus is 70 μg/mL, and against vesicular stomatitis virus, influenza A virus and measles virus is 100 μg/mL[3]. P-536 (10-200 μg/mL; 48 hours) effectively inhibits the production of HSV-1 infectious units in HeLa cells, with 10 μg/mL inhibiting 1 log unit and 50 μg/mL inhibiting 3 log units, and no cytotoxicity was observed at these concentrations[3]. In HSV-1-infected HeLa cells, the addition of P-536 (100 μg/mL) at the initial stage of infection inhibited viral protein synthesis, but the addition 5 hours after infection had no such effect [3]. P-536 (50-200 μg/mL; 2 hours) inhibited viral protein glycosylation in HSV-1-infected HeLa cells. Its inhibitory effect on mannose and galactose incorporation was stronger than its inhibitory effect on glucosamine, and the inhibitory effect was observed at all tested concentrations [3]. P-536 (10-100 μg/mL; 8 hours of pretreatment for RNA samples and 16 hours of pretreatment for DNA samples) completely inhibited the synthesis of HSV-1 TK mRNA in infected HeLa cells and significantly reduced the accumulation of HSV-1 DNA at a concentration of 100 μg/mL [3]. P-536 (100 μg/mL; 5 min; co-incubation with [3H]thymidine) blocked thymidine phosphorylation in HSV-1-infected HeLa cells, and dTMP was almost undetectable in the cellular nucleotide pool [3]. P-536 (150-200 μg/mL; 48 h (protein synthesis assay), 6 days (cell proliferation assay)) showed very low cytotoxicity in simulated infected HeLa cells: protein synthesis levels at 200 μg/mL were consistent with the control group, while the inhibitory effect on cell proliferation at 150 μg/mL was less than 0.5-log [3]. P-536 (5-10 μg/mL; 8-10 days) effectively inhibited the growth of extracellular Trypanosoma krusei epiflagellates in vitro, with an ID50 of less than 5 μg/mL on day 8 of culture [4]. P-536 (25 μg/mL; 3 days) inhibited the growth of Trypanosoma cruzi amastigotes in J774G8 cells, with an ID50 of 25 μg/mL on day 3 of culture [4]. P-536 (50 μg/mL; 4 days) repaired J774G8 cells infected with Trypanosoma cruzi: administration at the early stage of infection prevented parasite-induced cell death and restored normal cell growth, while administration 12 hours after infection reduced the infection load [4]. P-536 (10-100 μg/mL; 1 hour) inhibited macromolecule synthesis in Trypanosoma cruzi epimastigotes; the inhibitory effect on RNA synthesis was strongest at 100 μg/mL, but it did not cause significant plasma membrane leakage in Trypanosoma cruzi epimastigotes (only 17% 86Rb+ efflux) [4].

Cytotoxicity assay [3]
Cell Types: Sham-infected HeLa cells
Tested Concentrations: 150 μg/mL; 200 μg/mL
Incubation Duration: 6 days (cell proliferation); 48 hours (protein synthesis)
Experimental Results: After incubation at 200 μg/mL for 48 hours, protein synthesis did not decrease to below the control level. After incubation at 150 μg/mL for 6 days, cell proliferation inhibition rate was less than 0.5 log10.

[1]. P-536: Inhibition of the renin-angiotensin system reduces vascular oxidative stress and vascular dysfunction in insulin-resistant rats[J]. American Journal of Hypertension, 2005, 18(S4): 202A-202A.

[2]. P-536: Hypertensive subjects with increased leukocyte oxidative damage have shorter telomere DNA[J]. American Journal of Hypertension, 2002, 15(S3): 227A-227A.

[3]. Mode of action of a new type of UDP-glucose analog against herpesvirus replication. Antimicrob Agents Chemother. 1988;32(8):1257-1261.

[4]. Activity of P536, a UDP-glucose analog, against Trypanosoma cruzi. Antimicrob Agents Chemother. 1988;32(9):1412-1415.

93426-60-9

Typically exists as solids at room temperature

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

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

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.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*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).

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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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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).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)