产品
编 号：F746502
分子式：C31H24Cl2N4O4
分子量：587.45
分子式：C31H24Cl2N4O4
分子量：587.45
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CAS No: 1643372-83-1
产品详情
生物活性：
BMS-986143 is an orally active, reversible BTK inhibitor with an IC50 of 0.26 nM. BMS-986143 also inhibits TEC, BLK, BMX, TXK FGR, YES1, ITK with IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM,19 nM, 21 nM, respectively. BMS-986143 can be used for the research of autoimmune diseases.
体内研究：
BMS-986143 demonstrates desirable efficacy in mouse models of collagen-induced arthritis (CIA) and anticollagen antibody-induced arthritis (CAIA). BMS-986143 exhibits high oral bioavailability (mouse 100%, dog 82%) and moderate Cmax (mouse 4.3, dog 1.2 μM) following oral administration (mouse 6, dog 2 mg/kg). BMS-986143 exhibits long elimination half-lives (mouse 3.6, dog 7.9 h) due to moderate plasma clearance (8.6, 4.4 mL/min/kg respectively) combined with low volumes of distribution (1.8, 2.6 L/kg respectively) following intravenous administration (mouse 3.0, dog 1.0 mg/kg).Animal Model:DBA/1 male mice (8-10wk of age) bearing CIA model
Dosage:15 and 45 mg/kg
Administration:Oral gavage; BID
Result:15 and 45 mg/kg provided dose-dependent inhibition of observed clinical disease progression (63% and 80%, respectively), representing 17 and 19 h coverage of the mouse whole blood IC50 (130 nM).
体外研究：
BMS-986143 inhibits BTK with IC50s of 6.9±3.4 and 25±19 nM in Ramos cellular assay and the human whole blood assay, respectively.BMS-986143 provides potent inhibition of end points derived from IgG-containing immune complex low affinity activating Fcγ receptor signaling in peripheral blood mononuclear cells (PBMC) (IC50=2 nM).BMS-986143 inhibits the expression of CD63 on the surface of basophils in human whole blood, driven by FcεRI signaling (IC50 of 54 nM).BMS-986143 inhibits calcium flux in Ramos B Cells, proliferation of human peripheral B Cells, CD86 surface expression in peripheral B Cells, and TNFα from human PBMC Cells with IC50s of 7±3, 1±0.4, 1±0.5, and 2 nM, respectively.
BMS-986143 is an orally active, reversible BTK inhibitor with an IC50 of 0.26 nM. BMS-986143 also inhibits TEC, BLK, BMX, TXK FGR, YES1, ITK with IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM,19 nM, 21 nM, respectively. BMS-986143 can be used for the research of autoimmune diseases.
体内研究：
BMS-986143 demonstrates desirable efficacy in mouse models of collagen-induced arthritis (CIA) and anticollagen antibody-induced arthritis (CAIA). BMS-986143 exhibits high oral bioavailability (mouse 100%, dog 82%) and moderate Cmax (mouse 4.3, dog 1.2 μM) following oral administration (mouse 6, dog 2 mg/kg). BMS-986143 exhibits long elimination half-lives (mouse 3.6, dog 7.9 h) due to moderate plasma clearance (8.6, 4.4 mL/min/kg respectively) combined with low volumes of distribution (1.8, 2.6 L/kg respectively) following intravenous administration (mouse 3.0, dog 1.0 mg/kg).Animal Model:DBA/1 male mice (8-10wk of age) bearing CIA model
Dosage:15 and 45 mg/kg
Administration:Oral gavage; BID
Result:15 and 45 mg/kg provided dose-dependent inhibition of observed clinical disease progression (63% and 80%, respectively), representing 17 and 19 h coverage of the mouse whole blood IC50 (130 nM).
体外研究：
BMS-986143 inhibits BTK with IC50s of 6.9±3.4 and 25±19 nM in Ramos cellular assay and the human whole blood assay, respectively.BMS-986143 provides potent inhibition of end points derived from IgG-containing immune complex low affinity activating Fcγ receptor signaling in peripheral blood mononuclear cells (PBMC) (IC50=2 nM).BMS-986143 inhibits the expression of CD63 on the surface of basophils in human whole blood, driven by FcεRI signaling (IC50 of 54 nM).BMS-986143 inhibits calcium flux in Ramos B Cells, proliferation of human peripheral B Cells, CD86 surface expression in peripheral B Cells, and TNFα from human PBMC Cells with IC50s of 7±3, 1±0.4, 1±0.5, and 2 nM, respectively.
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