Bropirimine
Based on 2 publication(s) in Google Scholar
Bropirimine (U-54461; U-54461S; PNU-54461) is an orally active TLR7 agonist. Bropirimine inhibits RANKL-induced osteoclast differentiation of mouse bone marrow-derived macrophages (BMMs). Bropirimine exhibits dose-dependent direct inhibitory effects on colony formation of cultured KK-47 and 724 cells. Bropirimine can be used for the study of cancers and bone metabolic disorders such as osteoporosis.
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- Purity: 99.94%
- CAS No.: 56741-95-8
- 화학식: C10H8BrN3O
- 분자량:266.10
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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용액&용해도
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- References
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Publications Citing Use of MedChemExpress (MCE) Bropirimine
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Biological Activity
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TLR7 |
Bropirimine (0.3-30 μg/mL, 3 d) inhibits RANKL-induced osteoclast differentiation of mouse BMMs in a concentration-dependent manner[1].
Bropirimine (0.3-30 μg/mL, 3 d) suppresses the formation of resorption pits on dentin disks in mouse BMM cultures with RANKL and M-CSF, and significantly reduces mRNA expression of TRAP and NFATc1[1].
Bropirimine (1-30 μg/mL, 4 d) inhibits 1α,25(OH)2D3-induced osteoclast differentiation of mouse BMCs in co-cultures with mouse osteoblastic UAMS-32 cells in a concentration-dependent manner[1].
Bropirimine (1-30 μg/mL, 48 h) significantly suppresses 1α,25(OH)2D3-induced RANKL mRNA expression in mouse osteoblastic UAMS-32 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Renca cells (5 × 106) were implanted under the capsule of the left kidney via flank incision into 8-10-week-old female euthymic BALB/c mice[3]
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Dosage:100, 500, 1000, 2000 mg/kg
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Administration:p.o., once daily, 5 consecutive days, starting on day 1 post-tumor inoculation
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Result:Achieved tumor growth inhibition at the dose of 1000 and 2000 mg/kg.
Chemical Information
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CAS No. 56741-95-8
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Appearance Solid
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분자량 266.10
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화학식 C10H8BrN3O
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Color White to off-white
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SMILES
O=C1NC(N)=NC(C2=CC=CC=C2)=C1Br
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Synonyms
U-54461; U-54461S; PNU-54461
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (2)
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Journal Impact Factor
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Most Recent
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Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Nanomedicine
Improving lipid nanoparticles delivery efficiency of macrophage cells by using immunomodulatory small molecules. [Abstract]2025 Feb 3:64:102809. PMID: 39904398
용액&용해도
DMSO : 50 mg/mL (187.90 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 (7.82 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 (7.82 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.
순도&문서
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Data Sheet (276 KB)
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SDS (418 KB)
- English - EN (418 KB)
- Français - FR (418 KB)
- Deutsch - DE (418 KB)
- Norwegian - NO (418 KB)
- Español - ES (418 KB)
- Swedish - SV (418 KB)
- Italian - IT (418 KB)
- Korean - KR (418 KB)
- Portuguese - PT (418 KB)
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Handling Instructions (2659 KB)
References
[1]. Suzuki H, et al. Bropirimine inhibits osteoclast differentiation through production of interferon-β. Biochem Biophys Res Commun. 2015;467(1):146‐151. [Content Brief]
[2]. Tei Y, et al. In vitro antitumor activity of bropirimine against urinary bladder tumor cells. Anticancer Res. 2002 May-Jun;22(3):1667-71. [Content Brief]
[3]. Fujioka T, et al. Antitumor effects of oral administration of an interferon-inducing pyrimidinone, Bropirimine, on murine renal-cell carcinoma. Cancer Chemother Pharmacol. 1995;36(1):7-12. [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 | 3.7580 mL | 18.7899 mL | 37.5799 mL | 93.9496 mL |
| 5 mM | 0.7516 mL | 3.7580 mL | 7.5160 mL | 18.7899 mL | |
| 10 mM | 0.3758 mL | 1.8790 mL | 3.7580 mL | 9.3950 mL | |
| 15 mM | 0.2505 mL | 1.2527 mL | 2.5053 mL | 6.2633 mL | |
| 20 mM | 0.1879 mL | 0.9395 mL | 1.8790 mL | 4.6975 mL | |
| 25 mM | 0.1503 mL | 0.7516 mL | 1.5032 mL | 3.7580 mL | |
| 30 mM | 0.1253 mL | 0.6263 mL | 1.2527 mL | 3.1317 mL | |
| 40 mM | 0.0939 mL | 0.4697 mL | 0.9395 mL | 2.3487 mL | |
| 50 mM | 0.0752 mL | 0.3758 mL | 0.7516 mL | 1.8790 mL | |
| 60 mM | 0.0626 mL | 0.3132 mL | 0.6263 mL | 1.5658 mL | |
| 80 mM | 0.0470 mL | 0.2349 mL | 0.4697 mL | 1.1744 mL | |
| 100 mM | 0.0376 mL | 0.1879 mL | 0.3758 mL | 0.9395 mL |
Bropirimine Related Classifications
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