BIIB091|cas:2247614-80-6|西域试剂

BIIB091,99.96%

产品编号：Bellancom-139984| CAS NO：2247614-80-6| 分子式：C₂₈H₃₄N₁₀O₂| 分子量：542.64

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-139984		￥10900.00	杭州北京（现货）
Bellancom-139984		￥17500.00	杭州北京（现货）

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BIIB091

产品介绍

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。

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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%).

体内研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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%).

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (230.36 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8428 mL	9.2142 mL	18.4284 mL
5 mM	0.3686 mL	1.8428 mL	3.6857 mL
10 mM	0.1843 mL	0.9214 mL	1.8428 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.83 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.83 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.83 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.83 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明