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SP-187 (SP187; MON-DNJ; UV-4) is a novel and potent alpha-Glucosidase inhibitor, also acting as a host-targeted iminosugar with in vitro and in vivo antiviral activity against filovirus infections. SP187 is active against influenza and dengue in vivo.
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| ln Vitro |
Using a yield-plaque assay technique, the antiviral activity of iminosugar SP187 (UV-4) against EBOV and MARV is evaluated in vitro, and the IC50 is found. With an IC50 of 29.97 and 47.72 μM for EBOV and MARV, respectively, antiviral activity for SP187 is noted[1].
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| ln Vivo |
Using a mouse model of EBOV infection, the effectiveness of UV-5, the most potent iminosugar studied in vitro, and SP187 (UV-4), the active free base component of UV-4B, is first evaluated. In this work, oral gavage or IP injection of 10 or 100 mg/kg of SP187 or UV-5 is given to C57Bl/6 mice. Dosing began approximately one hour before to infection with 1000 pfu of mouse-adapted EBOV. For ten days, BID dosing was repeated at roughly 12-hour intervals for UV-5 or TID dosing at roughly 8-hour intervals for SP187. The chosen dosages and timing are derived on studies on mouse naïve tolerance. When comparing the iminosugar-treated mice to the vehicle control, no effectiveness is seen[1].
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| References |
[1]. Warfield KL, et al. Assessment of the potential for host-targeted iminosugars UV-4 and UV-5 activity against filovirus infections in vitro and in vivo. Antiviral Res. 2017 Feb;138:22-31
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| Molecular Formula |
C16H33NO5
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| Molecular Weight |
319.442
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| Exact Mass |
319.2359
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| CAS # |
615253-61-7
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| Related CAS # |
1333144-07-2 (HCl);615253-61-7;
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
O([H])[C@@]1([H])[C@@]([H])([C@]([H])(C([H])([H])N(C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])OC([H])([H])[H])[C@]1([H])C([H])([H])O[H])O[H])O[H]
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| Synonyms |
SP 187 MON-DNJ UV-4 SP187 MON DNJ UV4 SP-187
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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 (~313.05 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.83 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 (7.83 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 (7.83 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 | 3.1305 mL | 15.6524 mL | 31.3048 mL | |
| 5 mM | 0.6261 mL | 3.1305 mL | 6.2610 mL | |
| 10 mM | 0.3130 mL | 1.5652 mL | 3.1305 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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