BIIB091

价格： ￥4360

品牌：MedChemExpress(MCE) 品牌认证

货号：HY-139984

产品详情

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
species	T_1/2 (h)	AUC_inf (h•ng/mL)	CL (mL/min/kg)	CL %Q_H	V_dss (L/kg)	T_max (h)	C_max (ng/mL)	AUC_inf (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