| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
TLR1/TLR2 heterodimer. Diprovocim is a potent synthetic agonist that activates the human TLR1/TLR2 heterodimer.
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| ln Vitro |
Diprovocim (0.01-10000 nM; 4 hours) induces THP-1 cells (EC50=110 pM), human peripheral blood mononuclear cells (PBMC) (EC50=875 pM), and simulated peritoneal macrophages (EC50=1.3 nM). Diprovocim (5 nM in THP-1 cells, 500 nM in mouse peritoneal macrophages; 15-120 minutes) induces phosphorylation of IKKα, IKKβ, p38, JNK, and ERK [2]. ] and dendritic cells derived from bone marrow (BMDC) (EC50=6.7 nM) generate TNF in a dose-dependent manner. Apart from TNF, Diprovocim also causes BMDC to produce IL-6 [2].
Diprovocim is a potent TLR1/TLR2 agonist that elicits full agonist activity in human THP-1 cells with an EC₅₀ of 110 pM. It stimulates the release of TNF-α from mouse macrophages with an EC₅₀ of 1.3 nM. Its activity can be inhibited by anti-TLR1 or anti-TLR2 antibodies, confirming target specificity. |
| ln Vivo |
Similar levels of serum OVA waveform IgG were generated 14 days later by diprovocim (10 mg/kg), which functions as an adjuvant when combined with egg albumen (OVA; 100 μg) and injected excisionally [2]. Tumor growth rate can be markedly increased by /kg) combined with ovalbumin (OVA; 100 μg) and injected prior to B16-OVA cell vaccination [2].
Diprovocim induces dose-dependent TNF production in vivo. It exhibits significant potential as an immune adjuvant with anticancer and immunomodulatory effects. The compound activates immune responses through TLR1/TLR2 agonism, promoting the release of pro-inflammatory cytokines that can enhance antitumor immunity. |
| Enzyme Assay |
In vitro TLR1/TLR2 activation assays for diprovocim typically use reporter cell lines such as HEK293 cells transfected with TLR1, TLR2, and an NF-κB-driven reporter gene. Cells are treated with varying concentrations of the compound, and reporter gene activity (such as luciferase) is measured to determine EC₅₀ values. Alternatively, primary immune cells such as THP-1 cells are used, and cytokine production is measured by ELISA.
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: THP-1 cells and mouse peritoneal macrophages Tested Concentrations: 5 nM in THP-1, 500 nM in mouse peritoneal macrophages Incubation Duration: 15, 30, 60, 120 minutes Experimental Results: Induces phosphorylation of IKKα, IKKβ, p38, JNK and ERK, and degradation of IκBα. In vitro cell-based assays for diprovocim evaluate its ability to activate immune cells and induce cytokine production. Human THP-1 monocytic cells or primary mouse peritoneal macrophages are treated with varying concentrations of the compound, and TNF-α release is measured by ELISA. The specificity of the response can be confirmed using anti-TLR1 or anti-TLR2 blocking antibodies. |
| Animal Protocol |
Animal/Disease Models: WT or Tlr2−/− C57BL/ 6J mice [2]
Doses: 10 mg/kg Route of Administration: intramuscularinjection Experimental Results: Induced similar levels of serum OVA-specific IgG compared with intramuscularinjection of 100 μg OVA This level was Dramatically elevated compared to the levels induced by OVA-loaded immunity mixed with the drug. In vivo animal studies for diprovocim evaluate its immunomodulatory and anticancer effects. The compound is administered systemically, and immune activation is assessed by measuring cytokine levels in serum or tissue. In tumor models, the compound's ability to enhance antitumor immunity and inhibit tumor growth is evaluated, often in combination with other immunotherapies such as checkpoint inhibitors. |
| ADME/Pharmacokinetics |
Diprovocim has a molecular weight of approximately 520.56 g/mol. Detailed pharmacokinetic parameters such as absorption, distribution, metabolism, and excretion are not extensively reported in the provided literature. The compound is typically formulated for systemic administration in animal studies. Solubility and stability data are available from commercial suppliers.
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| Toxicity/Toxicokinetics |
Specific toxicity data for diprovocim is not extensively reported. As a TLR1/TLR2 agonist that induces pro-inflammatory cytokine production, potential toxicities may include systemic inflammatory responses if administered at high doses. The compound is classified as a research-grade chemical and is not intended for human use.
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| References |
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| Additional Infomation |
Diprovocim (CAS# 2170867-89-5) is a potent synthetic agonist of the TLR1/TLR2 heterodimer with an EC₅₀ of 110 pM in human THP-1 cells. It stimulates TNF-α release from mouse macrophages with an EC₅₀ of 1.3 nM. The compound has anticancer and immunomodulatory effects and exhibits significant potential as an immune adjuvant. Its activity is inhibited by anti-TLR1 or anti-TLR2 antibodies. It has not received FDA approval.
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| Molecular Formula |
C56H56N6O6
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|---|---|
| Molecular Weight |
909.0805
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| Exact Mass |
908.426
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| CAS # |
2170867-89-5
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| PubChem CID |
137553173
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| Appearance |
White to off-white solid powder
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| LogP |
5.3
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
68
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| Complexity |
1620
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| Defined Atom Stereocenter Count |
12
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| SMILES |
O=C([C@@]1([H])C([H])([H])N(C(C2C([H])=C([H])C(=C([H])C=2[H])C(N2C([H])([H])[C@]([H])(C(N([H])[C@]3([H])C([H])([H])[C@@]3([H])C3C([H])=C([H])C([H])=C([H])C=3[H])=O)[C@@]([H])(C(N([H])[C@]3([H])C([H])([H])[C@@]3([H])C3C([H])=C([H])C([H])=C([H])C=3[H])=O)C2([H])[H])=O)=O)C([H])([H])[C@]1([H])C(N([H])[C@]1([H])C([H])([H])[C@@]1([H])C1C([H])=C([H])C([H])=C([H])C=1[H])=O)N([H])[C@]1([H])C([H])([H])[C@@]1([H])C1C([H])=C([H])C([H])=C([H])C=1[H]
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| InChi Key |
ABZBNXFGYUSVCJ-UYMKNZQYSA-N
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| InChi Code |
InChI=1S/C56H56N6O6/c63-51(57-47-25-39(47)33-13-5-1-6-14-33)43-29-61(30-44(43)52(64)58-48-26-40(48)34-15-7-2-8-16-34)55(67)37-21-23-38(24-22-37)56(68)62-31-45(53(65)59-49-27-41(49)35-17-9-3-10-18-35)46(32-62)54(66)60-50-28-42(50)36-19-11-4-12-20-36/h1-24,39-50H,25-32H2,(H,57,63)(H,58,64)(H,59,65)(H,60,66)/t39-,40-,41-,42-,43-,44-,45-,46-,47+,48+,49+,50+/m1/s1
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| Chemical Name |
(3S,4S)-1-[4-[(3S,4S)-3,4-bis[[(1S,2R)-2-phenylcyclopropyl]carbamoyl]pyrrolidine-1-carbonyl]benzoyl]-3-N,4-N-bis[(1S,2R)-2-phenylcyclopropyl]pyrrolidine-3,4-dicarboxamide
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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 : ~33.33 mg/mL (~36.66 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (2.75 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 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 | 1.1000 mL | 5.5001 mL | 11.0001 mL | |
| 5 mM | 0.2200 mL | 1.1000 mL | 2.2000 mL | |
| 10 mM | 0.1100 mL | 0.5500 mL | 1.1000 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.
Link: https://clinicaltrials.gov/ct2/show/NCT06972134
Conditions:Cholesterol Gallstone DissolutionProducts are for research use only; We do not sell to patients
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