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KRN5 

Cat. No.: HY-112126 Purity: 98.49%
Handling Instructions

KRN5 is a Nuclear factor of activated T cells 5 (NFAT5) suppressor, with an IC50 of 750 nM.

For research use only. We do not sell to patients.

KRN5 Chemical Structure

KRN5 Chemical Structure

CAS No. : 1800465-47-7

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5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3300 In-stock
Estimated Time of Arrival: December 31
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  • Biological Activity

  • Protocol

  • Technical Information

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  • References

Description

KRN5 is a Nuclear factor of activated T cells 5 (NFAT5) suppressor, with an IC50 of 750 nM.

IC50 & Target

IC50: 750 nM (NFAT5)[1].

In Vitro

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].

In Vivo

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].

Solvent & Solubility
In Vitro: 

DMSO : < 1 mg/mL (insoluble or slightly soluble)

H2O : < 0.1 mg/mL (insoluble)

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Mice[1]
To induce adjuvant induced arthritis (AIA) in mice, 2 mg of complete Freund's adjuvant is injected intradermally to 8-week-old C57BL/6 mice. KRN2 (3 mg/kg) is given to AIA mice via daily peritoneal injection, and swelling in the ankle and footpad is measured for 2 weeks. To induce Collagen induced arthritis (CIA) in mice, 8-week-old DBA/1J mice are immunized with bovine type II collagen emulsified in CFA on day 0. On day 14, a booster injection of CII in incomplete Freund's adjuvant is given in the left footpad. After one week, KRN2 (3 mg/kg) is injected daily into the CIAmice. Other CII-immunized mice receive KRN5 orally (15 mg/kg and 60 mg/kg) on alternate days. Paws and ankles are harvested on day 40, and the degrees of inflammation, synovial proliferation, and bone destruction are evaluated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

459.47

Formula

C₂₇H₂₂FNO₅

CAS No.

1800465-47-7

SMILES

COC1=C(OC)C2=C(C=C1)C(CC3=CC=CC=C3F)=C4N(C2=O)CCC(C4=C5)=CC6=C5OCO6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
KRN5
Cat. No.:
HY-112126
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KRN5

Cat. No.: HY-112126