Description
KRN2 is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 100 nM. KRN2 has potential to treat NFAT5-mediated Chronic Arthritis.
Product information
CAS Number: 248260-75-5
Molecular Weight: 479.93
Formula: C27H23ClFNO4
Chemical Name: 21-[(2-fluorophenyl)methyl]-16,17-dimethoxy-5,7-dioxa-13λ⁵-azapentacyclo[11.8.0.0²,¹⁰.0⁴,⁸.0¹⁵,²⁰]henicosa-1(21),2,4(8),9,13,15,17,19-octaen-13-ylium chloride
Smiles: [Cl-].COC1C(=CC=C2C=1C=[N+]1CCC3=CC4OCOC=4C=C3C1=C2CC1=CC=CC=C1F)OC
InChiKey: RPHFGOXVJGNJJH-UHFFFAOYSA-M
InChi: InChI=1S/C27H23FNO4.ClH/c1-30-23-8-7-18-20(11-17-5-3-4-6-22(17)28)26-19-13-25-24(32-15-33-25)12-16(19)9-10-29(26)14-21(18)27(23)31-2;/h3-8,12-14H,9-11,15H2,1-2H3;1H/q+1;/p-1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
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:
KRN2 selectively suppresses the expression of pro-inflammatory genes, including Nos2 and Il6, without hampering high-salt-induced NFAT5 and its target gene expressions. KRN2 dose-dependently inhibits the NF-κB p65 binding to Nfat5 promoter 1 and directly blocks the interaction between NF-κB p65 and its DNA binding sequence in the upstream site (base pairs -3000 to +1) of Nfat5 exon 1.
In Vivo:
KRN2 (3 mg/kg, i.p., daily for 2 weeks) effectively suppresses AIA in which innate immune cells play a predominant role. KRN2 (3 mg/kg, i.p., daily) effectively suppresses CIA as well as AIA in mice, decreasing the production of pro-inflammatory cytokines and autoantibodies as well as macrophage infiltration.
Products are for research use only. Not for human use.
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