货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V57674-1ml	10mM in DMSO	￥21400.00 V57674-1ml ￥21400.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V57674-1ml

10mM in DMSO

￥21400.00

货期：3-5天

产品描述：

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.

体外研究：

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[1].

Pharmacokinetics of BIIB091 in preclinical species[1]

体内研究：

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.

参考文献：

1. Hopkins BT, et al. Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis. J Med Chem. 2021 Nov 4.

保存条件：

-80°C 6个月;-20°C 1个月

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.843 ml	9.214 ml	18.428 ml
5 mM	0.369 ml	1.843 ml	3.686 ml
10 mM	0.184 ml	0.921 ml	1.843 ml
50 mM	0.037 ml	0.184 ml	0.369 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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