CasNo.1242156-23-5,RN486,(1242156-23-5) Suppliers

1 Gram	Negotiable

Min.Order :1 Gram
Purity: 98% purity
Payment Terms : T/T,Other

Keywords

RN486 1242156-23-5 98% purity

Quick Details

Appearance:powder
Application:intermediate
PackAge:According to the need of packing
ProductionCapacity:100|Kilogram|Month
Storage:Sealed in dry,Room Temperature
Transportation:air,sea,courier

Superiority:

Product Name:   RN486
Synonyms:   RN486;6-cyclopropyl-8-fluoro-2-(2-(hydroxyMethyl)-3-(1-Methyl-5-((5-(4-Methylpiperazin-1-yl)pyridin-2-yl)aMiNA)-6-oxo-1,6-dihydropyridin-3-yl)phenyl)isoquiNAlin-1(2H)-one;6-cyclopropyl-8-fluoro-2-(2-(hydroxyMethyl)-3-(1-Methyl-5-(5-(4-Methylpiperazin-1-yl)pyridin-2-ylaMino)-6-oxo-1,6-dihydropyridin-3-yl)phenyl)isoquinolin-1(2H)-one;CS-689;RN486; RN-486; RN 486;RN486/RN-486;RN468;6-Cyclopropyl-2-[3-[1,6-dihydro-1-methyl-5-[[5-(4-methyl-1-piperazinyl)-2-pyridinyl]amino]-6-oxo-3-pyridinyl]-2-(hydroxymethyl)phenyl]-8-fluoro-1(2H)-isoquinolinone
CAS:   1242156-23-5
MF:   C35H35FN6O3
MW:   606.69
EINECS:   200-110-4
Product Categories:   Inhibitors
Mol File:   1242156-23-5.mol

Details:

Boiling point    868.6±65.0 °C(Predicted)
density    1.378±0.06 g/cm3(Predicted)
pka   13.95±0.10(Predicted)
CAS DataBase Reference   1242156-23-5

Biological activity   RN486 is an effective BTK inhibitor with an IC50 of 4 nM.
In vitro   RN486 not only potently and selectively inhibits the Btk enzyme, but also displays functional activities in human cell-based assays in multiple cell types, blocking Fcε receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC50 = 7.0 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC50 = 21.0 nM). RN486 is able to block the signaling of BCR as demonstrated by a marked inhibition of phosphorylation of both Btk and PLCγ2 in B cells. RN486 displays a selective B cell inhibitory profile in BioMAP Systems.
In vivo   RN486 displays similar functional activities in rodent models, effectively preventing type I and type III hypersensitivity responses. More importantly, RN486 produces robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 inhibits both joint and systemic inflammation either alone or in combination with methotrexate, reducing both paw swelling and inflammatory markers in the blood.