KRN5 |
Catalog No.GC31489
One-Click Copy Product Info
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KRN5, un derivado de KRN2, es un supresor activo oral del factor nuclear de células T activadas 5 (NFAT5), con una IC50 de 750 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1800465-47-7
Sample solution is provided at 25 µL, 10mM.
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KRN5 is a Nuclear factor of activated T cells 5 (NFAT5) suppressor, with an IC50 of 750 nM.
The plasma half-life of KRN5 is estimated at >8 h when KRN5 is administered orally, and the bioavailability (F%) after oral and intravenous administration was 15% in rats. The IC50 value of KRN5 is 0.75 μM as determined by NFAT5-dependent reporter assay in LPS-stimulated RAW 264.7 cells, suggesting that the in vitro NFAT5 inhibitory capacity can be maintained after chemical modification of KRN2 to KRN5. Moreover, KRN5 is less toxic than BBR as determined by a cytotoxicity assay, hERG K+ channel assay, cytochrome inhibition assay, and liver microsomal metabolic stability test. KRN5 at a concentration of 1 μM inhibits the expressions of NFAT5, IL-6, MCP-1, and GM-CSF, which are NFAT5 target molecules, in RAW264.7 macrophages stimulated with LPS[1].
It is found that oral feeding of KRN5 every other day for 3 weeks from day 21 dose-dependently mitigates arthritis severity. When compared to methotrexate, a commonly used DMARD, the efficacy of oral KRN5 at 60mg/kg is more potent in suppressing arthritis; a supra-therapeutic dose (5 mg/kg) of methotrexate is administered orally twice a week for the same experimental period. Of special interest, no side effects are noted throughout the course of our experiments. The concentration of serum anti-type II collagen IgG also significantly decrease in the sera of KRN5-treated mice. In parallel, TNF-α and IL-6 production by LPS-stimulated splenocytes are significantly lower in KRN5-treated CIA mice than in vehicle-treatedmice. NFAT5 expression in spleen cells stimulated by LPS is also reduced by KRN5[1].
[1]. Han EJ, et al. Suppression of NFAT5-mediated Inflammation and Chronic Arthritis by Novel κB-binding Inhibitors. EBioMedicine. 2017 Apr;18:261-273.
| Cas No. | 1800465-47-7 | SDF | |
| Canonical SMILES | COC1=C(OC)C2=C(C=C1)C(CC3=CC=CC=C3F)=C4N(C2=O)CCC(C4=C5)=CC6=C5OCO6 | ||
| Formula | C27H22FNO5 | M.Wt | 459.47 |
| Solubility | DMSO : 6 mg/mL (13.06 mM);Water : < 0.1 mg/mL (insoluble) | Storage | Store at -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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1764 mL | 10.8821 mL | 21.7642 mL |
| 5 mM | 435.3 μL | 2.1764 mL | 4.3528 mL |
| 10 mM | 217.6 μL | 1.0882 mL | 2.1764 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)