| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
KRN2 bromide targets NFAT5 (nuclear factor of activated T cells 5), a transcription factor. It is a selective inhibitor with an IC₅₀ of 100 nM (0.1 µM). The compound directly blocks the DNA binding region between NF-κB p65 and its Nfat5 exon 1 upstream site, dose-dependently suppressing NF-κB p65's binding to the Nfat5 promoter.
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| ln Vitro |
Without interfering with the high-salt-induced production of NFAT5 and its target genes, KRN2 specifically suppresses the expression of pro-inflammatory genes, such as Nos2 and Il6 [1]. KRN2 directly blocks the DNA binding region between NF-κB p65 and its Nfat5 exon 1 upstream site (base pairs -3000 to +1) and dose-dependently suppresses NF-κB p65's binding to Nfat5 promoter 1. exchanges [1].
In vitro, KRN2 specifically suppresses the expression of pro-inflammatory genes, such as Nos2 and Il6, without interfering with the high-salt-induced production of NFAT5 and its target genes. It shows much stronger inhibition of NFAT5-dependent reporter activity in RAW 264.7 macrophages than BBR, with an IC₅₀ of 0.1 µM for KRN2 compared to 4 µM for BBR. |
| ln Vivo |
AIA, in which innate immune cells predominate, can be successfully inhibited by KRN2 (3 mg/kg, intraperitoneal injection, once day, for two weeks) [1]. In mice, CIA and AIA can be efficiently inhibited by KRN2 (3 mg/kg, intraperitoneal injection, daily), which also decreases the generation of pro-inflammatory cytokines, autoantibodies, and macrophage infiltration [1].
In vivo, KRN2 bromide effectively inhibits antigen-induced arthritis (AIA), which is predominantly mediated by innate immune cells. In mouse models, KRN2 (3 mg/kg, intraperitoneal injection, daily for two weeks) effectively inhibits AIA and collagen-induced arthritis (CIA), decreasing the production of pro-inflammatory cytokines, autoantibodies, and macrophage infiltration. |
| Enzyme Assay |
In vitro binding assays measure the compound's ability to inhibit the interaction between NF-κB p65 and the Nfat5 promoter. These assays typically involve electrophoretic mobility shift assays (EMSA) or chromatin immunoprecipitation (ChIP) to assess DNA binding.
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| Cell Assay |
In vitro cell-based assays use RAW 264.7 macrophages to evaluate the inhibition of NFAT5-dependent reporter activity. Cells are treated with KRN2, and reporter gene expression is measured to determine the IC₅₀. The expression of pro-inflammatory genes like Nos2 and Il6 is also measured.
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| Animal Protocol |
Animal/Disease Models: 8weeks old C57BL/6 mice were intradermally injected with 2 mg of Freund's complete adjuvant [1].
Doses: 3 mg/kg. Doses: intraperitoneal (ip) injection daily for 2 weeks Experimental Results: Effectively inhibits AIA. Animal/Disease Models: 8weeks old DBA/1J mice were immunized with bovine type II collagen [1]. Doses: 3 mg/kg. Mode of Route of Administration: Daily intraperitoneal (ip) injection. Experimental Results: Effectively inhibited CIA and AIA in mice and diminished the production of pro-inflammatory cytokines and autoantibodies as well as macrophage infiltration. In vivo animal studies are conducted in mouse models of arthritis, such as AIA and CIA. KRN2 bromide is administered via intraperitoneal injection at a dose of 3 mg/kg daily. Endpoints include assessment of joint inflammation, measurement of pro-inflammatory cytokines and autoantibodies, and evaluation of macrophage infiltration. |
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of KRN2 bromide have not been detailed in the provided search results. However, its efficacy in vivo following intraperitoneal administration suggests it reaches sufficient systemic concentrations.
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| Toxicity/Toxicokinetics |
The toxicity profile of KRN2 bromide has not been detailed in the provided search results. It is supplied as a light yellow to yellow solid powder with a purity of ≥98%.
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| References | |
| Additional Infomation |
KRN2 bromide is also known as KRN2 (bromide). The related CAS number for the free base is 248260-75-5. The product is for research use only and is not for human use.
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| Molecular Formula |
C27H23BRFNO4
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| Molecular Weight |
524.378230333328
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| Exact Mass |
523.079
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| CAS # |
1390654-28-0
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| Related CAS # |
KRN2;248260-75-5
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| PubChem CID |
71611938
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
34
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| Complexity |
681
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(C1C=CC=CC=1F)C1C2=CC=C(OC)C(OC)=C2C=[N+]2CCC3=CC4OCOC=4C=C3C=12.[Br-]
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| InChi Key |
UMRLOOJWWLJVCD-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C27H23FNO4.BrH/c1-30-23-8-7-18-20(11-17-5-3-4-6-22(17)28)26-19-13-25-24(32-15-33-25)12-16(19)9-10-29(26)14-21(18)27(23)31-2;/h3-8,12-14H,9-11,15H2,1-2H3;1H/q+1;/p-1
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| Chemical Name |
21-[(2-fluorophenyl)methyl]-16,17-dimethoxy-5,7-dioxa-13-azoniapentacyclo[11.8.0.02,10.04,8.015,20]henicosa-1(13),2,4(8),9,14,16,18,20-octaene;bromide
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~18.33 mg/mL (~34.96 mM)
H2O : ~1.1 mg/mL (~2.10 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.83 mg/mL (3.49 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 18.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.83 mg/mL (3.49 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 18.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.83 mg/mL (3.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9070 mL | 9.5351 mL | 19.0701 mL | |
| 5 mM | 0.3814 mL | 1.9070 mL | 3.8140 mL | |
| 10 mM | 0.1907 mL | 0.9535 mL | 1.9070 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.
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