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.
Product information
CAS Number: 1800465-47-7
Molecular Weight: 459.47
Formula: C27H22FNO5
Chemical Name: 21-[(2-fluorophenyl)methyl]-16,17-dimethoxy-5,7-dioxa-13-azapentacyclo[11.8.0.0²,¹⁰.0⁴,⁸.0¹⁵,²⁰]henicosa-1(21),2,4(8),9,15,17,19-heptaen-14-one
Smiles: COC1=C2C(=O)N3CCC4=CC5OCOC=5C=C4C3=C(CC3=CC=CC=C3F)C2=CC=C1OC
InChiKey: WSIOACCDMOKVNM-UHFFFAOYSA-N
InChi: InChI=1S/C27H22FNO5/c1-31-21-8-7-17-19(11-16-5-3-4-6-20(16)28)25-18-13-23-22(33-14-34-23)12-15(18)9-10-29(25)27(30)24(17)26(21)32-2/h3-8,12-13H,9-11,14H2,1-2H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 6 mg/mL (13.06 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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.
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. 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.
Products are for research use only. Not for human use.
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