[CAS NO. 1800465-47-7] KRN5

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PRODUCTS SPECIFICATIONS [1800465-47-7]

Catalog

HY-112126

Brand

MCE

CAS

1800465-47-7

DESCRIPTION [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

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

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

In Vitro:

DMSO : 5 mg/mL ( 10.88 mM ; ultrasonic and warming and heat to 80°C)

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.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: 0.5 mg/mL (1.09 mM); Suspended solution; Need ultrasonic
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

* All of the co-solvents are available by MCE.

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.

Synonyms

8H-Benzo[g]-1,3-benzodioxolo[5,6-a]quinolizin-8-one, 13-[(2-fluorophenyl)methyl]-5,6-dihydro-9,10-dimethoxy-