Physicochemical Properties
| Molecular Formula | C23H20F3N5O |
| Molecular Weight | 439.43 |
| Appearance | Typically exists as solids at room temperature |
| HS Tariff Code | 2934.99.9001 |
| 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) |
Biological Activity
| Targets | TLR7 TLR8 |
| ln Vitro | PVP-037.2 (0.1-100 μM, 24 hours) induces TNF and IL-1β production in human aged peripheral blood mononuclear cells (PBMCs) in a concentration-dependent manner [1]. PVP-037.2 (100 μM, 20-24 hours) has TLR7/8-dependent immunomodulatory properties [1]. |
| ln Vivo | PVP-037.2 (3 mg/kg, intravenous injection, measured 0-8 hours after administration) has a high plasma clearance rate and almost no hemolytic activity in C57BL/6J adult mice (weight 20 to 30 g) [1]. PVP-037.2 (100 nmol per mouse, intravenous injection, single immunization) has a strong adjuvant effect in C57BL/6J mice vaccinated with trivalent recombinant rHA influenza vaccine Flublok and SARS-CoV-2 spike protein [1]. PVP-037.2 O/W emulsion formulation (10 nmol per mouse, intravenous injection, IgG titer measured on day 42) can enhance the innate immune activation ability of wild-type C57BL/6J mice compared with PVP-037.2 alone [1]. |
| Animal Protocol |
Animal/Disease Models: WT C57BL/6J mice Doses: 10 nmol per mouse Route of Administration: Intravenous injection (i.v.), single injection Experimental Results: Significantly enhanced total IgG and IgG2c class-switched antibody responses (IgG titers measured on day 42). Animal/Disease Models: C57BL/6J mice (6 to 8 weeks old, stimulated with the trivalent recombinant rHA influenza vaccine Flublok and the SARS-CoV-2 spike protein) Doses: 100 nmol per mouse Route of Administration: Intravenous injection (i.v.), single injection Experimental Results: Resulted that the production of antigen-specific IgG1 and IgG2c was significantly enhanced in C57BL/6J mice stimulated with the trivalent recombinant rHA influenza vaccine Flublok (IgG titers measured on day 28) and the SARS-CoV-2 spike protein (IgG titers measured on day 42). |
| References |
[1]. Soni D, et al. From hit to vial: Precision discovery and development of an imidazopyrimidine TLR7/8 agonist adjuvant formulation[J]. Science Advances, 2024, 10(27): eadg3747. |
Solubility Data
| Solubility (In Vitro) | 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 |
| 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 (e.g. IP/IV/IM/SC) 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). 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) 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). 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 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2757 mL | 11.3784 mL | 22.7568 mL | |
| 5 mM | 0.4551 mL | 2.2757 mL | 4.5514 mL | |
| 10 mM | 0.2276 mL | 1.1378 mL | 2.2757 mL |