KRN5
- Product Name
- KRN5
- CAS No.
- 1800465-47-7
- Chemical Name
- KRN5
- Synonyms
- KRN5;KRN5,KRN-5;KRN5, 10 mM in DMSO;13-(2-Fluorobenzyl)-9,10-dimethoxy-5,6-dihydro-8H-[1,3]dioxolo[4,5-g]isoquinolino[3,2-a]isoquinolin-8-one;8H-Benzo[g]-1,3-benzodioxolo[5,6-a]quinolizin-8-one, 13-[(2-fluorophenyl)methyl]-5,6-dihydro-9,10-dimethoxy-
- CBNumber
- CB84796664
- Molecular Formula
- C27H22FNO5
- Formula Weight
- 459.47
- MOL File
- 1800465-47-7.mol
KRN5 Property
- Boiling point:
- 682.0±55.0 °C(Predicted)
- Density
- 1.42±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 6 mg/mL (13.06 mM);Water : < 0.1 mg/mL (insoluble)
- form
- Solid
- pka
- -1.93±0.40(Predicted)
- color
- Light yellow to yellow
KRN5 Chemical Properties,Usage,Production
Uses
KRN5, a derivative of KRN2, is an oral active Nuclear factor of activated T cells 5 (NFAT5) suppressor, with an IC50 of 750 nM. KRN5 has potential to treat NFAT5-mediated Chronic Arthritis[1].
in vivo
Oral feeding of KRN5 (15 mg/kg and 60 mg/kg) every other day for 3 weeks from day 21 dose-dependently mitigates arthritis severity[1].
The concentration of serum anti-type II collagen IgG also significantly decreases in the sera of KRN5-treated mice. TNF-α and IL-6 production by LPS-stimulated splenocytes are significantly lower in KRN5-treated CIA mice than in vehicle-treated mice[1].
| Animal Model: | 8-week-old DBA/1Jmice immunized with bovine type II collagen[1]. |
| Dosage: | 15 mg/kg and 60 mg/kg. |
| Administration: | Orally on alternate days (every other day) for 3 weeks. |
| Result: | Dose-dependently mitigated arthritis severity. |
References
[1] Han EJ, et al. Suppression of NFAT5-mediated Inflammation and Chronic Arthritis by Novel κB-binding Inhibitors. EBioMedicine. 2017 Apr;18:261-273. DOI:10.1016/j.ebiom.2017.03.039
KRN5 Preparation Products And Raw materials
Raw materials
Preparation Products
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