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Inosine pranobex (Imunovir; Delimmun; Groprinosin), a combinatinon of inosine, acetamidobenzoic acid, and dimethylaminoisopropanol, is a novel, potent, broad-spectrum antiviral agent potentially useful for HIV/AIDs infection. Inosine pranobex is also an immunopotentiator/immunostimulant, and has no direct effect on viral cells.
| Targets |
- T lymphocytes: Enhances proliferation induced by mitogens (PHA, Con A) at concentrations 10-150 μg/ml; the immunopotentiator here is Inosine pranobex (Imunovir; Delimmun; Groprinosin) [1]
- Suppressor T cells: Induces suppressor cell activity at 0.1-100 μg/ml concentrations; the active agent is Inosine pranobex (Imunovir; Delimmun; Groprinosin) [1] |
|---|---|
| ln Vitro |
1. Lymphocyte proliferation assay:
- Inosine pranobex (Imunovir; Delimmun; Groprinosin) (10-150 μg/ml) significantly enhanced PHA- or Con A-induced proliferation of mouse spleen lymphocytes, but had no effect on unstimulated cells [1] - Optimal concentration for Inosine pranobex (Imunovir; Delimmun; Groprinosin): 10-100 μg/ml [1] - On human lymphocytes: Inosine pranobex (Imunovir; Delimmun; Groprinosin) enhanced proliferative response to mitogens (ConA, PWM) in 3-7 day cultures [1] 2. Suppressor cell induction: - Inosine pranobex (Imunovir; Delimmun; Groprinosin) added to mouse lymphocyte cultures (0.1-100 μg/ml) induced suppressor cells that inhibited mixed lymphocyte reactions to same extent as Con A-activated suppressors [1] - The suppressor activity induced by Inosine pranobex (Imunovir; Delimmun; Groprinosin) was T-cell dependent (abolished by anti-Thy 1.2 serum) [1] |
| ln Vivo |
1. Antibody response enhancement:
- Dose-dependent effect of Inosine pranobex (Imunovir; Delimmun; Groprinosin): 50 μg/kg to 50 mg/kg (i.p.) significantly increased numbers of IgM antibody-forming cells in mouse spleen when administered at immunization time or 7-day pretreatment [1] - Oral administration of Inosine pranobex (Imunovir; Delimmun; Groprinosin): <500 mg/kg/day given at or 1 day after immunization stimulated immune responses [1] - High dose effect of Inosine pranobex (Imunovir; Delimmun; Groprinosin): LD₅₀ (5 g/kg) or pretreatment did not impair immune responsiveness [1] 2. Contact sensitivity: - 50 mg/kg (i.p.) of Inosine pranobex (Imunovir; Delimmun; Groprinosin) increased ear swelling in mice sensitized with trinitro-chlorobenzene [1] |
| Cell Assay |
1. Lymphocyte proliferation (for Inosine pranobex (Imunovir; Delimmun; Groprinosin) evaluation):
- Mouse spleen cells: Cultured in RPMI-1640 with 5% FCS, antibiotics [1] - Experimental setup: - 1×10⁶ responder cells/well + 1×10⁶ mitomycin-treated stimulator cells (for MLR) [1] - Incubated 72 h, pulsed with 1 μCi tritiated thymidine for final 16 h [1] - Harvested and counted radioactivity (cpm) to assess effect of Inosine pranobex (Imunovir; Delimmun; Groprinosin) [1] - Inosine pranobex (Imunovir; Delimmun; Groprinosin) addition: Filter-sterilized drug added at 0.1-1000 μg/ml final concentration [1] 2. Suppressor cell assay (for Inosine pranobex (Imunovir; Delimmun; Groprinosin) evaluation): - Activation phase: 2×10⁷ splenocytes cultured 3 days with Inosine pranobex (Imunovir; Delimmun; Groprinosin) (0.1-1000 μg/ml) or Con A (3 μg/ml) [1] - Effector phase: Treated cells mitomycin C-treated (to prevent proliferation) and added (2×10⁵ cells/well) to responder cultures to measure suppressor activity induced by Inosine pranobex (Imunovir; Delimmun; Groprinosin) [1] |
| Animal Protocol |
1. Antibody response study (for Inosine pranobex (Imunovir; Delimmun; Groprinosin)):
- Mice: BALB/c or C57BL/6, female [1] - Immunization: i.v. sheep red blood cells (SRBC) [1] - Inosine pranobex (Imunovir; Delimmun; Groprinosin) administration: - i.p. at 0.5 μg/kg to 5 g/kg at immunization time or 7 days pretreatment [1] - Oral: <500 mg/kg/day at or 1 day after immunization [1] - Assessment: 4-5 days post-immunization, spleen antibody-forming cells counted by hemolytic plaque assay to evaluate Inosine pranobex (Imunovir; Delimmun; Groprinosin) effect [1] 2. Contact sensitivity study (for Inosine pranobex (Imunovir; Delimmun; Groprinosin)): - Sensitization: Mice painted with picryl chloride on abdomen [1] - Challenge: 5-7 days later, ear painted with same hapten [1] - Inosine pranobex (Imunovir; Delimmun; Groprinosin) administration: 50 mg/kg i.p. given either at sensitization or challenge [1] - Measurement: Ear swelling 24 h post-challenge to assess Inosine pranobex (Imunovir; Delimmun; Groprinosin) activity [1] |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Rapidly absorbed from the gastrointestinal tract. Excreted in urine. Biological Half-Life 50 minutes |
| Toxicity/Toxicokinetics |
1. Acute toxicity of inosine pranobec (Imunovir; Delimmun; Groprinobec): - Mouse LD₅₀: 5 g/kg (intraperitoneal injection) [1] - Rat LD₅₀: 9150 mg/kg (oral administration) [1] 2. Chronic toxicity of inosine pranobec (Imunovir; Delimmun; Groprinobec): - No immunosuppressive effect was observed even at high doses [1]
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| References | |
| Additional Infomation |
Inosine planobilizer (isoprostinosine or methylisoprostinosine) is a compound preparation composed of inosine, acetaminobenzoic acid, and dimethylaminoisopropanol, used as an antiviral drug. Inosine planobilizer is a preparation containing inosine, 4-acetaminobenzoic acid, and N,N-dimethylaminoisopropanol, possessing immunomodulatory and antiviral activity. Although its exact mechanism of action is not fully understood, inosine planobilizer appears to have the effects of a thymosin analogue; after administration, the drug may induce T cell differentiation and enhance the lymphoproliferative response against transformed or virus-infected cells. Inosine is an alkylamino alcohol complex used to treat a variety of viral infections. Unlike other antiviral drugs, its mechanism of action is through modulating or stimulating cell-mediated immune processes, rather than acting directly on the virus.
Drug Indications Inosine planobilizer is also indicated for the treatment of mucocutaneous infections caused by herpes simplex virus (types 1 and 2), and as adjunctive therapy to podophyllotoxin or carbon dioxide laser for the treatment of genital warts. Mechanism of Action Inosine pranobec stimulates cell-mediated immune processes to combat viral infections. Pharmacodynamics It works by slowing the growth and spread of viruses in the body. It can also stimulate the human immune system, thereby enhancing the body's ability to resist these infections. 1. Chemical properties of inosine pranobec (Imunovir; Delimmun; Groprinobec): - Inosine pranobec (Imunovir; Delimmun; Groprinobec) = Inosine + N,N-dimethylamino-2-propanol para-acetaminobenzoate (molar ratio 1:3) [1] 2. Mechanism of action of inosine pranobec (Imunovir; Delimmun; Groprinobec): - Immunostimulatory effect: Inosine pranobec (Imunovir; Delimmun; Groprinobec) can enhance the response of T cells to mitogens and antigens without affecting unstimulated cells [1] |
| Molecular Formula |
C52H78N10O17
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|---|---|
| Molecular Weight |
1115.23
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| Exact Mass |
1114.554
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| Elemental Analysis |
C, 56.00; H, 7.05; N, 12.56; O, 24.39
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| CAS # |
36703-88-5
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| Related CAS # |
36703-88-5 (pranobex);141684-35-7 (phosphoramidite);58-63-9;
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| PubChem CID |
135449284
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| Appearance |
White to off-white solid powder
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| Boiling Point |
732.8ºC at 760 mmHg
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| Flash Point |
397ºC
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| LogP |
1.766
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| Hydrogen Bond Donor Count |
13
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| Hydrogen Bond Acceptor Count |
22
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
79
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| Complexity |
658
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O1[C@]([H])(C([H])([H])O[H])[C@]([H])([C@]([H])([C@]1([H])N1C([H])=NC2C(N([H])C([H])=NC1=2)=O)O[H])O[H].O([H])C([H])(C([H])([H])[H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H].O([H])C([H])(C([H])([H])[H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H].O([H])C([H])(C([H])([H])[H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H].O([H])C(C1C([H])=C([H])C(=C([H])C=1[H])N([H])C(C([H])([H])[H])=O)=O.O([H])C(C1C([H])=C([H])C(=C([H])C=1[H])N([H])C(C([H])([H])[H])=O)=O.O([H])C(C1C([H])=C([H])C(=C([H])C=1[H])N([H])C(C([H])([H])[H])=O)=O
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| InChi Key |
YLDCUKJMEKGGFI-QCSRICIXSA-N
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| InChi Code |
InChI=1S/C10H12N4O5.3C9H9NO3.3C5H13NO/c15-1-4-6(16)7(17)10(19-4)14-3-13-5-8(14)11-2-12-9(5)18;3*1-6(11)10-8-4-2-7(3-5-8)9(12)13;3*1-5(7)4-6(2)3/h2-4,6-7,10,15-17H,1H2,(H,11,12,18);3*2-5H,1H3,(H,10,11)(H,12,13);3*5,7H,4H2,1-3H3/t4-,6-,7-,10-;;;;;;/m1....../s1
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| Chemical Name |
4-acetamidobenzoic acid compound with 9-((2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-1,9-dihydro-6H-purin-6-one and 1-(dimethylamino)propan-2-ol (3:1:3)
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| Synonyms |
Inosine pranobex; NP113; NP-113; NP 113
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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 (~56.04 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (1.87 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 20.8 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: ≥ 2.08 mg/mL (1.87 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 20.8 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: ≥ 2.08 mg/mL (1.87 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 | 0.8967 mL | 4.4834 mL | 8.9668 mL | |
| 5 mM | 0.1793 mL | 0.8967 mL | 1.7934 mL | |
| 10 mM | 0.0897 mL | 0.4483 mL | 0.8967 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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