产品
编 号：F750501
分子式：C28H34N10O2
分子量：542.64
分子式：C28H34N10O2
分子量：542.64
产品类型
规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 2247614-80-6
产品详情
生物活性：
BIIB091 is a potent, selective, orally active and reversible BTK inhibitor, with an IC50 of <0.5 nM. BIIB091 binds the BTK protein to sequester TYR-551 into an inactive conformation with excellent affinity. BIIB091 can be used for the research of multiple sclerosis.
体内研究：
BIIB091 (0.03-30 mg/kg; p.o. twice daily for 10 d) reduces the anti-NP IgM antibody titers (88%, 77%, 59%, 59%, 44%, 34%, and 22%) in the TI-2 immunization model.Pharmacokinetics of BIIB091 in preclinical speciesspeciesIV (1 mg/kg)PO(5 mg/kg) in HMPC/Tween
T1/2 (h)AUCinf (h?ng/mL)CL (mL/min/kg)CL %QHVdss (L/kg)Tmax (h)Cmax (ng/mL)AUCinf (h?ng/mL)%F
rat2.174810220.40.9693152242
cyno1.194318440.70.331104144631
dog6.0167512331.71.61440607589
Animal Model:C57BL/6 mice immunized with NP-Ficoll a thymus-independent type 2 (TI-2) antigen
Dosage:0.03, 0.1, 0.3, 1, 10, 30 mg/kg in a CMC/Tween suspension formulation
Administration:P.o. twice daily for 10 days
Result:Observed a significant reduction of the anti-NP IgM antibody titers (88%, 77%, 59%, 59%, 44%, 34%, and 22%).
体外研究：
BIIB091 inhibits the phosphorylation of PLCγ2 in the Ramos human B-cell line, with an IC50 of 6.9 nM.BIIB091 blocks anti-IgM-stimulated CD69 activation in PBMCs with an IC50 of 6.9 nM.BIIB091 inhibits FcγR-induced ROS production in purified primary neutrophils, with an IC50 of 4.5 nM.BIIB091 inhibits FcγRI and FcγRIII-mediated TNFα secretion upon simulation with FcγR agonists such as coated human IgG (all FcγR, IC50=5.6 nM), anti-CD16 (FcγRIII, IC50=8.0 nM), anti-CD64 (FcγRI IC50=3.1 nM), and cross-linked anti-CD16 (FcγRIII IC50=1.3 nM) in human monocytes.BIIB091 inhibits the phosphorylation of BTK (IC50=24 nM) and blocks both BCR mediated B cell and FcεR-induced basophil activation as measured by inhibition of CD69 and CD63 expression (IC50=71 nM and IC50=82 nM, respectively) in the whole blood assays.
BIIB091 is a potent, selective, orally active and reversible BTK inhibitor, with an IC50 of <0.5 nM. BIIB091 binds the BTK protein to sequester TYR-551 into an inactive conformation with excellent affinity. BIIB091 can be used for the research of multiple sclerosis.
体内研究：
BIIB091 (0.03-30 mg/kg; p.o. twice daily for 10 d) reduces the anti-NP IgM antibody titers (88%, 77%, 59%, 59%, 44%, 34%, and 22%) in the TI-2 immunization model.Pharmacokinetics of BIIB091 in preclinical speciesspeciesIV (1 mg/kg)PO(5 mg/kg) in HMPC/Tween
T1/2 (h)AUCinf (h?ng/mL)CL (mL/min/kg)CL %QHVdss (L/kg)Tmax (h)Cmax (ng/mL)AUCinf (h?ng/mL)%F
rat2.174810220.40.9693152242
cyno1.194318440.70.331104144631
dog6.0167512331.71.61440607589
Animal Model:C57BL/6 mice immunized with NP-Ficoll a thymus-independent type 2 (TI-2) antigen
Dosage:0.03, 0.1, 0.3, 1, 10, 30 mg/kg in a CMC/Tween suspension formulation
Administration:P.o. twice daily for 10 days
Result:Observed a significant reduction of the anti-NP IgM antibody titers (88%, 77%, 59%, 59%, 44%, 34%, and 22%).
体外研究：
BIIB091 inhibits the phosphorylation of PLCγ2 in the Ramos human B-cell line, with an IC50 of 6.9 nM.BIIB091 blocks anti-IgM-stimulated CD69 activation in PBMCs with an IC50 of 6.9 nM.BIIB091 inhibits FcγR-induced ROS production in purified primary neutrophils, with an IC50 of 4.5 nM.BIIB091 inhibits FcγRI and FcγRIII-mediated TNFα secretion upon simulation with FcγR agonists such as coated human IgG (all FcγR, IC50=5.6 nM), anti-CD16 (FcγRIII, IC50=8.0 nM), anti-CD64 (FcγRI IC50=3.1 nM), and cross-linked anti-CD16 (FcγRIII IC50=1.3 nM) in human monocytes.BIIB091 inhibits the phosphorylation of BTK (IC50=24 nM) and blocks both BCR mediated B cell and FcεR-induced basophil activation as measured by inhibition of CD69 and CD63 expression (IC50=71 nM and IC50=82 nM, respectively) in the whole blood assays.
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