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- 2025年12月05日
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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- 规格：
10 mM * 1 mL///1 mg
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BIIB091
CAS No. : 2247614-80-6
MCE 国际站：BIIB091
产品活性：BIIB091 是一种有效，选择性，具有口服活性和可逆的 BTK 抑制剂，IC50 值 <0.5 nM。BIIB091 与 BTK 蛋白结合，将 Tyr-551 隔离成具有出色亲和力的非活性构象。 BIIB091 可用于多发性硬化症的研究。
研究领域：Protein Tyrosine Kinase/RTK
作用靶点：Btk
In Vitro: 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.
In Vivo: 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 species
| species | IV (1 mg/kg) | PO (5 mg/kg) in HMPC/Tween | |||||||
| T1/2 (h) | AUCinf (h•ng/mL) | CL (mL/min/kg) | CL %QH | Vdss (L/kg) | Tmax (h) | Cmax (ng/mL) | AUCinf (h•ng/mL) | %F | |
| rat | 2.1 | 748 | 10 | 22 | 0.4 | 0.9 | 693 | 1522 | 42 |
| cyno | 1.1 | 943 | 18 | 44 | 0.7 | 0.33 | 1104 | 1446 | 31 |
| dog | 6.0 | 1675 | 12 | 33 | 1.7 | 1.6 | 1440 | 6075 | 89 |
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文献和实验11.2(10.0-80.0)1.59±0.341.67±0.38(0.50-2.65)135±12.0128±14.0(78.0-155)19.2±4.9317.6±4.36(13.1-29.5)2.65±0.882.62±0.87(1.00-4.30)146±1.15141±1.40(138-155)5.75±0.206.40±0.16(3.60-6.80)101±1.45105±1.22(92.0-122)24.2±3.1522.8±3.20(16.2-31.8)4.82±1.055.06±
步骤 a. 样品制备 ( 蛋白提取 ) (1) 细胞培养 、处理和收集; (2) 将细胞在 IEF 裂解缓冲液中溶解; (3) 将样品离心以去除不溶的细胞碎片和 DNA ，提取上清， -80 ℃保存。 b. 蛋白质定量和上样 (1) 固相 PH 梯度干胶条 (Immobi-line PH Gradient ， IPG) 水化、等电聚焦; (2)IPG 的平衡; (3)SDS-PAGE ;
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