Diprovocim-1 |
Katalog-Nr.GC48352
One-Click Copy Product Info
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Diprovocim-1 is a TLR1/TLR2 agonist, with EC50 values of 0.11nM and 1.3nM in THP-1 cells and mouse macrophages, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2170867-89-5
Sample solution is provided at 25 µL, 10mM.
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Diprovocim-1 is a TLR1/TLR2 agonist, with EC50 values of 0.11nM and 1.3nM in THP-1 cells and mouse macrophages, respectively[1]. Diprovocim-1 induces the formation of TLR2/TLR1 heterodimers as well as TLR2 homodimers in vitro[2]. Diprovocim-1 has been widely used as an adjuvant in combination with anti-PD-L1 therapy to eliminate melanoma in mice[3].
In vitro, Diprovocim-1 treatment (10nM) for 4h significantly enhanced the levels of tumor necrosis factor (TNF) in mouse peritoneal macrophages [4].
In vivo, a single intraperitoneal injection of Diprovocim-1 (10mg/kg) and ovalbumin (OVA) (5mg/kg) for 14 days significantly increased the levels of OVA-specific circulating antibodies of different subtypes in serum of C57BL/6J mice[5]. Diprovocim-1 (10mg/kg) administered intraperitoneally to C57BL/6 mice at 18h and 2h before 12Gy total body irradiation (TBI) significantly ameliorated radiation-induced intestinal injury, reduced leukocyte loss, and alleviated body weight loss[6].
References:
[1] Morin M D, Wang Y, Jones B T, et al. Diprovocims: a new and exceptionally potent class of toll-like receptor agonists[J]. Journal of the American Chemical Society, 2018, 140(43): 14440-14454.
[2] Su L, Wang Y, Wang J, et al. Structural basis of TLR2/TLR1 activation by the synthetic agonist diprovocim[J]. Journal of medicinal chemistry, 2019, 62(6): 2938-2949.
[3] Hu H G, Li Y M. Emerging adjuvants for cancer immunotherapy[J]. Frontiers in Chemistry, 2020, 8: 601.
[4] Wang Y, Su L, Morin M D, et al. Adjuvant effect of the novel TLR1/TLR2 agonist Diprovocim synergizes with anti–PD-L1 to eliminate melanoma in mice[J]. Proceedings of the National Academy of Sciences, 2018, 115(37): E8698-E8706.
[5] Yang M H, Russell J L, Mifune Y, et al. Next-generation diprovocims with potent human and murine TLR1/TLR2 agonist activity that activate the innate and adaptive immune response[J]. Journal of medicinal chemistry, 2022, 65(13): 9230-9252.
[6] Fang D, Zhao H, Pei L, et al. Diprovocim protects against the radiation-induced damage via the TLR2 signaling pathway[J]. Molecular Medicine, 2025, 31(1): 139.
| Cell experiment [1]: | |
Cell lines | Mouse peritoneal macrophages |
Preparation Method | Mouse peritoneal macrophages were cultured in DMEM medium containing 10% v/v fetal bovine serum (1% v/v penicillin and streptomycin) at 37°C in 95% air /5% CO2. Cells were seeded in 96-well plates at a density of 1×105 cells per well and stimulated with Diprovocim-1 (0.01, 0.1, 1, 10, and 100nM) for 4 hours. Levels of TNF in cells were measured. |
Reaction Conditions | 0.01, 0.1, 1, 10, and 100nM; 4h |
Applications | Diprovocim-1 treatment significantly enhanced the levels of TNF of mouse peritoneal macrophages in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female C57BL/6J mice |
Preparation Method | Female 8-week-old C57BL/6J mice (approximately 20g) were intravenously injected with vehicle (DMSO:Tween 80:saline = 1:1:8) on day 0. Saline = 1:1:1.8) (n=8), vehicle mixed with OVA (5mg/kg) (n=8), or OVA (5mg/kg) was further mixed with Diprovocim-1 (10mg/kg) (n=8) per mouse. On day 14, the titers of OVA-specific IgG, IgG1, or IgG2b in the serum of the mice were measured. |
Dosage form | 10mg/kg for once; i.p. |
Applications | Diprovocim-1 treatment enhanced the levels of OVA-specific IgG, IgG1, or IgG2b in the mice. |
References: | |
| Cas No. | 2170867-89-5 | SDF | |
| Canonical SMILES | O=C(C1=CC=C(C=C1)C(N2C[C@@H](C(N[C@@H]3[C@](C4=CC=CC=C4)([H])C3)=O)[C@H](C(N[C@@H]5[C@](C6=CC=CC=C6)([H])C5)=O)C2)=O)N7C[C@@H](C(N[C@@H]8[C@](C9=CC=CC=C9)([H])C8)=O)[C@H](C(N[C@@H]%10[C@](C%11=CC=CC=C%11)([H])C%10)=O)C7 | ||
| Formula | C56H56N6O6 | M.Wt | 909.1 |
| Löslichkeit | DMSO : 33.33 mg/mL (36.66 mM; ultrasonic and warming and heat to 60°C); H2O : < 0.1 mg/mL (insoluble) | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.1 mL | 5.4999 mL | 10.9999 mL |
| 5 mM | 220 μL | 1.1 mL | 2.2 mL |
| 10 mM | 110 μL | 550 μL | 1.1 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)