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[CAS NO. 1800465-47-7] KRN5
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-112126 |
| Brand: | MCE |
| CAS: | 1800465-47-7 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 459.47 |
| Molecular Formula | C27H22FNO5 |
| SMILES | COC1=C(OC)C2=C(C=C1)C(CC3=CC=CC=C3F)=C4N(C2=O)CCC(C4=C5)=CC6=C5OCO6 |
Summary
KRN5, a derivative of KRN2, is an oral active Nuclear factor of activated T cells 5 (NFAT5) suppressor, with an IC 50 of 750 nM. KRN5 has potential to treat NFAT5-mediated Chronic Arthritis [1] .
IC50 & Target
IC50: 750 nM (NFAT5) [1] .
In Vitro
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, which makes it a potential drug candidate
[1]
.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 5 mg/mL ( 10.88 mM ; ultrasonic and warming and heat to 80°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1764 mL | 10.8821 mL | 21.7642 mL |
| 5 mM | 0.4353 mL | 2.1764 mL | 4.3528 mL |
| 10 mM | 0.2176 mL | 1.0882 mL | 2.1764 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 0.5 mg/mL (1.09 mM); Suspended solution; Need ultrasonic
Synonyms
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