2. Immunology/Inflammation Apoptosis MAPK/ERK Pathway NF-κB
  3. Toll-like Receptor (TLR) TNF Receptor p38 MAPK NF-κB
  4. Diprovocim

Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC50=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC50=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses.

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Diprovocim Chemical Structure

Diprovocim Chemical Structure

CAS No. : 2170867-89-5

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Customer Review

Based on 5 publication(s) in Google Scholar

Diprovocim Related Antibodies

Top Publications Citing Use of Products

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TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

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TNFRSF1A/CD120a TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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p38 MAPK p38α p38β MAPK13 p38δ p38γ

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC50=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC50=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses[1][2].

IC50 & Target[1][2]

TLR1

 

TLR2

 

p38 MAPK

 

NF-κB

 

Cellular Effect
Cell Line Type Value Description References
THP-1 EC50
110 pM
Compound: Diprovocim
Agonist activity at TLR1/2 in human THP-1 cells assessed as increase in TNF-alpha release incubated for 4 hrs by ELISA
Agonist activity at TLR1/2 in human THP-1 cells assessed as increase in TNF-alpha release incubated for 4 hrs by ELISA
[PMID: 30852386]
In Vitro

Diprovocim (5 nM in THP-1 and 500 nM in mouse peritoneal macrophage; 15-120 mins) induces phosphorylation of IKKα, IKKβ, p38, JNK, and ERK, as well as degradation of IκBα in THP-1 cells and mouse peritoneal macrophages[2].
Diprovocim (0.01-10000 nM; 4 hours) induces dose-dependent TNF production by THP-1 cells (EC50=110 pM) and human peripheral blood mononuclear cells (PBMC) (EC50=875 pM) and by mouse peritoneal macrophages (EC50=1.3 nM) and bone marrow-derived dendritic cells (BMDC) (EC50=6.7 nM). In addition to TNF, Diprovocim induced IL-6 production by mouse BMDC[2].

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

Diprovocim Related Antibodies

Western Blot Analysis[2]

Cell Line: THP-1 cells and mouse peritoneal macrophages
Concentration: 5 nM in THP-1 and 500 nM in mouse peritoneal macrophages
Incubation Time: 15, 30, 60, 120 mins
Result: Induced phosphorylation of IKKα, IKKβ, p38, JNK, and ERK, as well as degradation of IκBα.
In Vivo

Diprovocim (10 mg/kg) uses as an adjuvant and mixed with ovalbumin (OVA; 100 μg) by i.m. induces similar levels of serum OVA-specific IgG after 14 days[2].
Diprovocim (10 mg/kg; i.m.) mixed with ovalbumin (OVA; 100 μg) before inoculation with B16-OVA cells immunizes significantly slows tumor growth rate but failed to prolong survival relative to OVA alone after 7 days[2].

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

Animal Model: WT or Tlr2−/− C57BL/6J mice[2]
Dosage: 10 mg/kg
Administration: IM
Result: Induced similar levels of serum OVA-specific IgG, which were highly elevated compared with levels induced by immunization with OVA plus vehicle by i.m. with 100 μg OVA mixed with this drug.
Molecular Weight

909.08

Formula

C56H56N6O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C[C@@H](C(N[C@@H]2[C@@H](C3=CC=CC=C3)C2)=O)[C@H](C(N[C@@H]4[C@@H](C5=CC=CC=C5)C4)=O)C1)C6=CC=C(C(N7C[C@@H](C(N[C@@H]8[C@@H](C9=CC=CC=C9)C8)=O)[C@H](C(N[C@@H]%10[C@@H](C%11=CC=CC=C%11)C%10)=O)C7)=O)C=C6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (36.66 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)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1000 mL 5.5001 mL 11.0001 mL
5 mM 0.2200 mL 1.1000 mL 2.2000 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

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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    90% Corn Oil

    Solubility: 2.5 mg/mL (2.75 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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
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 1.1000 mL 5.5001 mL 11.0001 mL 27.5003 mL
5 mM 0.2200 mL 1.1000 mL 2.2000 mL 5.5001 mL
10 mM 0.1100 mL 0.5500 mL 1.1000 mL 2.7500 mL
15 mM 0.0733 mL 0.3667 mL 0.7333 mL 1.8334 mL
20 mM 0.0550 mL 0.2750 mL 0.5500 mL 1.3750 mL
25 mM 0.0440 mL 0.2200 mL 0.4400 mL 1.1000 mL
30 mM 0.0367 mL 0.1833 mL 0.3667 mL 0.9167 mL
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Diprovocim Related Classifications

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.

Keywords:

Diprovocim2170867-89-5Toll-like Receptor (TLR)TNF Receptorp38 MAPKNF-κBTumor Necrosis Factor ReceptorTNFRNuclear factor-κBNuclear factor-kappaBTLR1/TLR2THP-1macrophagesadjuvantimmune responsesBMDCIKKαIKKβp38JNKERKovalbuminInhibitorinhibitorinhibit

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