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Purity: ≥98%
Loviride, formerly known as R-89439, is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and a RNA-directed DNA polymerase inhibitor potentially for the treatment of HIV infection. It has an IC50 of 0.3 µM for reverse transcriptase from HIV-1. Loviride (R 89439) inhibits HIV-1, HIV-2 and SIV replication in MT-4 cells.
| Targets |
Reverse transcriptase (IC50 = 0.3 µM); NNRTI
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|---|---|
| ln Vitro |
In MT-4 cells, loviride (0.01 µM) suppresses HIV-1(IIIB) replication as well as HIV-2 and SIV. The EC50 for HIV-2 (ROD), HIV-2 (EHO), and HIV-2 (ROD) is 85.5 µM and 7.4 µM, respectively. SIV (mndGB1), SIV (mac251), and SIV (agm3) are, in that order, 11.4, 28.5, and 57.0 µM [1].
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| Enzyme Assay |
Objective: To investigate whether, in addition to HIV-1, different strains of HIV-2 (ROD and EHO) and SIV (mac251, agm3 and mndGB1) are sensitive to a selection of NNRTI i.e. delavirdine, the HEPT derivative I-EBU (MKC-442), 8-chloro-TIBO (tivirapine), alpha-APA (Loviride), nevirapine and the pyridinone derivative L-697,661.
Methods and results: The NNRTI tested inhibited the replication of the different strains of HIV-2 and SIV at micromolar concentrations. The inhibitory effects of the NNRTI on HIV-2-induced cytopathicity correlated well with their inhibitory effects on HIV-2 RT activity. Drug-resistant HIV-2 (EHO) variants containing the Ser102Leu and/or Glu219Asp mutations in their RT were selected after passaging the virus in MT-4 cells in the presence of increasing concentrations of delavirdine. The EHO virus mutants were at least 20-fold less susceptible to the antiviral effects of delavirdine. Some cross-resistance, depending on the mutant strain, was observed with the other NNRTI tested (i.e. MKC-442, tivirapine, Loviride and pyridinone L-697,661). Conclusions: Our data demonstrate that NNRTI are not exclusively specific for HIV-1 but are also inhibitory to different HIV-2 and SIV strains. These observations will have important implications for the development of new NNRTI with higher activity against both HIV-1 and HIV-2. Furthermore, in view of their anti-SIV activity, NNRTI could be evaluated further for their in vivo anti-retrovirus efficacy in non-human primate models [1]. |
| References | |
| Additional Infomation |
Loviride is an organic molecular entity.
After the initial discovery of 1-(2-hydroxyethoxymethyl)-6-(phenylthio)thymine (HEPT) and tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and thione (TIBO) derivatives, several other non-nucleoside reverse transcriptase (RT) inhibitors (NNRTI), including nevirapine (BI-RG-587), pyridinone derivatives (L-696,229 and L-697,661), delavirdine (U-90152), alpha-anilinophenylacetamides (alpha-APA) and various other classes of NNRTI have been described. The hallmark of NNRTI has been based on their ability to interact with a specific site ('pocket') of HIV-1 RT.[1] |
| Molecular Formula |
C17H16CL2N2O2
|
|---|---|
| Molecular Weight |
351.22714
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| Exact Mass |
350.059
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| Elemental Analysis |
C, 58.14; H, 4.59; Cl, 20.19; N, 7.98; O, 9.11
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| CAS # |
147362-57-0
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| PubChem CID |
3963
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.354g/cm3
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| Boiling Point |
550.3ºC at 760mmHg
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| Melting Point |
226.3 °C
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| Flash Point |
286.6ºC
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| Vapour Pressure |
3.69E-12mmHg at 25°C
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| Index of Refraction |
1.637
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| LogP |
5.365
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
23
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| Complexity |
436
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CJPLEFFCVDQQFZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H16Cl2N2O2/c1-9-6-7-11(10(2)22)14(8-9)21-16(17(20)23)15-12(18)4-3-5-13(15)19/h3-8,16,21H,1-2H3,(H2,20,23)
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| Chemical Name |
2-((2-acetyl-5-methylphenyl)amino)-2-(2,6-dichlorophenyl)acetamide
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| Synonyms |
R-89439; R 89439; R89439; loviride; 147362-57-0; 2-(2-acetyl-5-methylanilino)-2-(2,6-dichlorophenyl)acetamide; CHEMBL37624; 3S1R1LZ09H; 2-((2-acetyl-5-methylphenyl)amino)-2-(2,6-dichlorophenyl)acetamide; R 089439; R089439.
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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 : ~62.5 mg/mL (~177.95 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (17.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 62.5 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8471 mL | 14.2357 mL | 28.4714 mL | |
| 5 mM | 0.5694 mL | 2.8471 mL | 5.6943 mL | |
| 10 mM | 0.2847 mL | 1.4236 mL | 2.8471 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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