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KRN5 

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

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.

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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10 mM * 1 mL in DMSO USD 88 In-stock
Estimated Time of Arrival: December 31
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100 mg USD 910 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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].

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].

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.
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

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
In Vitro: 

DMSO : 6 mg/mL (13.06 mM; Need ultrasonic)

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
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KRN5
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HY-112126
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