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Purity: ≥98%
Tomeglovir (also known as BAY-38-4766) is a novel, potent and non-nucleoside anti-CMV (cytomegalovirus) agent which inhibits processing of viral DNA-concatemers with IC50s of 0.34 μM and 0.039 μM for HCMV and MCMV. Tomeglovir protects against cytomegalovirus (CMV) disease and mortality in immunocompromised guinea pigs. Tomeglovir-resistant HCMV and MCMV strains are not cross-resistant to the nucleoside analogues ganciclovir and cidofovir or the pyrophosphate analogue foscarnet, indicating a different mode of action. Tomeglovir is highly specific for the viral as opposed to cellular functions, since UL89 is related to a bacteriophage terminase and no human equivalent exists.
| Targets |
HCMV(IC50= 0.34 μM);HCMV(MCMV=0.039 μM)
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|---|---|
| ln Vitro |
Strong anti-CMV agent tomeglovir (BAY 38-4766) has IC50 values for HCMV and MCMV of 0.34 μM and 0.039 μM, respectively. Additionally, HELF and NIH 3T3 cells are suppressed by tomeglovir, with CC50s of 85 μM and 62.5 μM, respectively[1]. At EC50s of 1.03 ± 0.57 μM and less than 1 μM, tomeglovir (BAY 38-4766) inhibits the HCMV Davis and different strains of monkey CMV[2].
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| ln Vivo |
Tomeglovir (BAY 38-4766; 3, 10, 30, 100 mg/kg, p.o.) decreases MCMV-DNA in the salivary glands, livers, and kidneys of NOD-SCID mice infected with MCMV in a dose-dependent manner while also extending the mice's survival. In the hollow fiber mouse model, tomeglovir (10, 25 and 50 mg/kg) exhibits antiviral activity[1]. In SCID mice infected with MCMV, tomeglovir (BAY 38-4766) exhibits antiviral activity; in rats and mice, the LD50 is greater than 2000 mg/kg[2].
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| Cell Assay |
A total of 100 μL of EMEM/10 is added to each well of 96-well microtitre plates to assess the toxicity of the drugs. Following the addition of 2 μL of 50 mM Tomeglovir stock solutions in duplicate into 198 μL in row 2, 100 μL up to row 12 and 100 μL of a HELF, NHDF, or 3T3 cell suspension (5 × 103 cells/mL) are added per well in a series of two-fold dilutions.Row 1 is the control cell that has not been treated. Following a 6-day incubation period at 37°C and 5% CO2, the cells are rinsed once with phosphate-buffered saline (PBS) and 200 μL of fluorescein diacetate, a fluorescent dye solution containing 10 μg/mL in PBS at pH 7.2, are added to each well. A Fluorskan Ascent fluorimeter (emission filter: 530 ± 15 nm, excitation filter: 485 ± 11 nm) is used to measure the fluorescence signal after 45 minutes. CC50 values are calculated graphically, and the relative fluorescence units (RFUs) of treated cells are expressed as percentages of untreated cell controls[2].
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| Animal Protocol |
Mice [1]
Avertin 2.5% (0.015-0.017 mL/g body weight) is used to anesthetize NOD/LtSz-scid/j mice weighing 20–30 g. Avertin 100% is made up of 10 g tribromoethyl alcohol in 10 mL tertiary amyl alcohol. The abdomens are opened and the fibers are inserted intra-abdominally after the belly has been shaved and cleaned aseptically. Two layers of sutures are used to close the abdomens. In this study, only asymptomatic animals are involved. The mice receive Tomeglovir treatment at the recommended dosages twice a day for four days in a row starting the day after transplantation. Under these circumstances, day 5 viral peak titers are seen in preliminary experiments[1]. |
| References |
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| Molecular Formula |
C23H27N3O4S
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|---|---|
| Molecular Weight |
441.54318
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| Exact Mass |
441.172
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| Elemental Analysis |
C, 62.56; H, 6.16; N, 9.52; O, 14.49; S, 7.26
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| CAS # |
233254-24-5
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| PubChem CID |
475330
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.667
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| LogP |
2.8
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
31
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| Complexity |
711
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)(CO)C(NC1=CC=C(NS(=O)(C2=C3C=CC=C(N(C)C)C3=CC=C2)=O)C=C1)=O
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| InChi Key |
OSQAKHSYTKBSPB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H27N3O4S/c1-23(2,15-27)22(28)24-16-11-13-17(14-12-16)25-31(29,30)21-10-6-7-18-19(21)8-5-9-20(18)26(3)4/h5-14,25,27H,15H2,1-4H3,(H,24,28)
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| Chemical Name |
N-(4-(((5-(Dimethylamino)-1-naphthyl)sulfonyl)amino)phenyl)-3-hydroxy-2,2-dimethylpropionamide
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| Synonyms |
Tomeglovir; BAY-38-4766; BAY 38-4766; BAY38-4766; BAY-384766; BAY 384766; BAY384766; BAY-38,4766; BAY 38,4766; BAY38,4766.
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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 : ≥ 108 mg/mL (~244.60 mM)
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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 | 2.2648 mL | 11.3240 mL | 22.6480 mL | |
| 5 mM | 0.4530 mL | 2.2648 mL | 4.5296 mL | |
| 10 mM | 0.2265 mL | 1.1324 mL | 2.2648 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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