Britannin
Based on 1 publication(s) in Google Scholar
Britannin is an NLRP3 inhibitor with an IC50 of 3.630 μM, exhibiting anti-inflammatory activity. Britannin inhibits the activation and assembly of the NLRP3 inflammasome by blocking the interaction between NLRP3 and NEK7. Additionally, Britannin demonstrates antitumor activity by inhibiting the proliferation of tumor cells through blocking the interaction between HIF-1α and Myc, thereby suppressing PD-L1 expression and enhancing cytotoxic T lymphocyte activity. Britannin can also induce apoptosis and autophagy in liver cancer cells by activating ROS-regulated AMPK. Britannin holds promise for research in the fields of anti-inflammatory and antitumor therapeutics.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 33627-28-0
- Formula: C19H26O7
- Molecular Weight:366.41
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) Britannin
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Biological Activity
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NLRP3 3.630 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | IC50 |
0.11 μM
Compound: 6
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Inhibition of LPS-induced NO production in mouse RAW264.7 cells measured after 24 hrs
Inhibition of LPS-induced NO production in mouse RAW264.7 cells measured after 24 hrs
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[PMID: 20515062] |
Britannin (1, 5, 10 μM, 30 min) inhibits NLRP3-mediated pyroptosis in mouse macrophages[4].
Britannin (1, 5, 10 μM, 30 min) inhibits activation of the NLRP3 inflammasome in an NF-κB-independent manner[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Bone marrow-derived macrophages(BMDMs)
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Concentration:1, 5, 10 μM
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Incubation Time:30 min
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Result:Dose-dependently inhibited secretion of the cleaved Caspase-1 and the mature IL-1β, and suppressed NLRP3-mediated pyroptosis in murine macrophages.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Monosodium urate (HY-B2130A) -induced gouty arthritis mouse model, Lipopolysaccharides (LPS) (HY-D1056) -induced acute lung injury mouse model[4]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection (i.p.), inject for three consecutive days (acute lung injury mouse model) or once every other day, for a total of 3 injections (Monosodium urate (HY-B2130A) -induced gouty arthritis mouse model)
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Result:Significantly suppressed the changes in footpad joint size, alleviated the migration of inflammatory cells in Monosodium urate (HY-B2130A) -induced gouty arthritis mouse model and nhibited the secretion of IL-1β and the activation of Caspase-1, demonstrating that Britannin prevented gouty arthritis through anti-inflammatory effects.
Suppressed pulmonary edema, breakdown of the pneumatic blood barrier, and cell infiltration in lung tissues and pathological injury and inflammatory cell infiltration in lung tissues, were ameliorated by Britannin treatment.
Chemical Information
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CAS No. 33627-28-0
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Appearance Solid
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Molecular Weight 366.41
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Formula C19H26O7
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Color White to off-white
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SMILES
C[C@]12[C@@]([C@@H](C[C@@](O3)([H])[C@](C(C3=O)=C)([H])[C@@H]2OC(C)=O)C)([H])[C@@H](OC(C)=O)C[C@@H]1O
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Exp Ther Med
Britannin inhibits cell proliferation, migration and glycolysis by downregulating KLF5 in lung cancer. [Abstract]2024 Jan 22;27(3):109. PMID: 38361511
Solvent & Solubility
DMSO : 250 mg/mL (682.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.68 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.68 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Cui YQ The suppressive effects of Britannin (Bri) on human liver cancer through inducing apoptosis and autophagy via AMPK activation regulated by ROS. Biochem Biophys Res Commun. 2018 Mar 11;497(3):916-923. [Content Brief]
[2]. Park HH, et al. Britanin suppresses LPS-induced nitric oxide, PGE2 and cytokine production via NF-κB and MAPK inactivation in RAW 264.7 cells. Int Immunopharmacol. 2013 Feb;15(2):296-302. [Content Brief]
[3]. Moghadam MH, et al. Anti-proliferative activity and apoptotic potential of britannin, a sesquiterpene lactone from Inula aucheriana. Nat Prod Commun. 2012 Aug;7(8):979-80. [Content Brief]
[4]. Shao, Jj., Li, Wf., Sun, Jf. et al. Britannin as a novel NLRP3 inhibitor, suppresses inflammasome activation in macrophages and alleviates NLRP3-related diseases in mice. Acta Pharmacol Sin, 2024, 45, 803–814. [Content Brief]
[5]. Zhang YF, et al. Britannin stabilizes T cell activity and inhibits proliferation and angiogenesis by targeting PD-L1 via abrogation of the crosstalk between Myc and HIF-1α in cancer. Phytomedicine. 2021 Jan;81:153425. [Content Brief]
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 (protect from light). 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 | 2.7292 mL | 13.6459 mL | 27.2918 mL | 68.2296 mL |
| 5 mM | 0.5458 mL | 2.7292 mL | 5.4584 mL | 13.6459 mL | |
| 10 mM | 0.2729 mL | 1.3646 mL | 2.7292 mL | 6.8230 mL | |
| 15 mM | 0.1819 mL | 0.9097 mL | 1.8195 mL | 4.5486 mL | |
| 20 mM | 0.1365 mL | 0.6823 mL | 1.3646 mL | 3.4115 mL | |
| 25 mM | 0.1092 mL | 0.5458 mL | 1.0917 mL | 2.7292 mL | |
| 30 mM | 0.0910 mL | 0.4549 mL | 0.9097 mL | 2.2743 mL | |
| 40 mM | 0.0682 mL | 0.3411 mL | 0.6823 mL | 1.7057 mL | |
| 50 mM | 0.0546 mL | 0.2729 mL | 0.5458 mL | 1.3646 mL | |
| 60 mM | 0.0455 mL | 0.2274 mL | 0.4549 mL | 1.1372 mL | |
| 80 mM | 0.0341 mL | 0.1706 mL | 0.3411 mL | 0.8529 mL | |
| 100 mM | 0.0273 mL | 0.1365 mL | 0.2729 mL | 0.6823 mL |
- Britannin
- 33627-28-0
- Apoptosis
- Autophagy
- NOD-like Receptor (NLR)
- Pyroptosis
- Bone marrow-derived macrophages(BMDMs)
- Monosodium urate (HY-B2130A) -induced gouty arthritis mouse model
- Lipopolysaccharides (LPS) (HY-D1056) -induced acute lung injury mouse model
- Anti-inflammatory activity
- Anti-tumor activity
- Arthritis
- Inhibitor
- inhibitor
- inhibit