1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)
  3. PVP-037.2

PVP-037.2 is a TLR7/8 agonist. PVP-037.2 can serve as an adjuvant to enhance vaccine-induced TH1 type immune responses, increasing the production of antigen-specific antibodies IgG1 and IgG2c.

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PVP-037.2

PVP-037.2 Chemical Structure

CAS No. : 3049666-32-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
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Description

PVP-037.2 is a TLR7/8 agonist. PVP-037.2 can serve as an adjuvant to enhance vaccine-induced TH1 type immune responses, increasing the production of antigen-specific antibodies IgG1 and IgG2c[1].

IC50 & Target

TLR7

 

TLR8

 

In Vitro

PVP-037.2 (0.1-100 μM, 24 h) induces concentration-dependent production of TNF and IL-1β in human elder peripheral blood mononuclear cells (PBMCs)[1].
PVP-037.2 ((100 μM, 20-24 h) demonstrates a TLR7/8-dependent immunomodulatory profile[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PVP-037.2 (3 mg/kg, i.v., measured 0-8 hours post-administration) shows high plasma clearance and almost no hemolytic activity in adult C57BL/6J mice (20 to 30 g in weight)[1].
PVP-037.2 (100 nmol per mouse, i.v., single immunization) exhibits potent adjuvant effects in C57BL/6J mice immunized with the trivalent recombinant rHA influenza vaccine Flublok and SARS-CoV-2 spike protein[1].
Compared with the use of PVP-037.2 alone, the PVP-037.2 O/W emulsion formulation (10 nmol per mouse, i.v., IgG titer measured on day 42) enhances the innate immune activation capability in wild-type C57BL/6J mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: WT C57BL/6J mice
Dosage: 10 nmol per mouse
Administration: Intravenous injection (i.v.), single injection
Result: Significantly enhanced total IgG and IgG2c class-switched antibody responses (IgG titers measured on day 42).
Animal Model: C57BL/6J mice (6 to 8 weeks old, stimulated with the trivalent recombinant rHA influenza vaccine Flublok and the SARS-CoV-2 spike protein)
Dosage: 100 nmol per mouse
Administration: Intravenous injection (i.v.), single injection
Result: 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).
Molecular Weight

439.43

Formula

C23H20F3N5O

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

CC1=CN2C=C(N=C2N=C1)C3=CC(NC(C4=C(C=C(C=C4)CN)C(F)(F)F)=O)=C(C=C3)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (227.57 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.18%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2757 mL 11.3784 mL 22.7568 mL 56.8919 mL
5 mM 0.4551 mL 2.2757 mL 4.5514 mL 11.3784 mL
10 mM 0.2276 mL 1.1378 mL 2.2757 mL 5.6892 mL
15 mM 0.1517 mL 0.7586 mL 1.5171 mL 3.7928 mL
20 mM 0.1138 mL 0.5689 mL 1.1378 mL 2.8446 mL
25 mM 0.0910 mL 0.4551 mL 0.9103 mL 2.2757 mL
30 mM 0.0759 mL 0.3793 mL 0.7586 mL 1.8964 mL
40 mM 0.0569 mL 0.2845 mL 0.5689 mL 1.4223 mL
50 mM 0.0455 mL 0.2276 mL 0.4551 mL 1.1378 mL
60 mM 0.0379 mL 0.1896 mL 0.3793 mL 0.9482 mL
80 mM 0.0284 mL 0.1422 mL 0.2845 mL 0.7111 mL
100 mM 0.0228 mL 0.1138 mL 0.2276 mL 0.5689 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
PVP-037.2
Cat. No.:
HY-159102
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