规格

价格

库存

数量

5 mg

¥ 278

现货

10 mg

¥ 393

现货

25 mg

¥ 659

现货

50 mg

¥ 978

现货

100 mg

¥ 1,470

现货

500 mg

¥ 4,150

现货

1 mL x 10 mM (in DMSO)

¥ 349

现货

生物活性

产品描述	Baricitinib phosphate (INCB028050) is a selective orally bioavailable JAK1/JAK2 inhibitor.
靶点活性	JAK1:5.9 nM, JAK3:560 nM, JAK2:5.7 nM, Tyk2:53 nM
体外活性	在细胞基础实验中，Baricitinib (INCB028050) 显示出强大的JAK信号传导和功能的抑制作用。在PBMCs中，Baricitinib 抑制了由IL-6刺激的典型底物STAT3 (pSTAT3)的磷酸化和随后的趋化因子MCP-1的产生，其IC50值分别为44 nM和40 nM。在分离的天真T细胞中，INCB028050 同样抑制了由IL-23刺激的pSTAT3（IC50=20 nM）。重要的是，这种抑制阻止了由Th17细胞生产的两种病原性细胞因子（IL-17和IL-22）的产生，Th17细胞是具有明显炎症和病原性特征的辅助T细胞亚型，其IC50值为50 nM。与此形成鲜明对比的是，结构相似但无效的JAK1/2抑制剂INCB027753和INCB029843在浓度高达10 μM的测试中，在任何这些实验系统中均无显著效果[1]。
体内活性	Baricitinib (INCB028050) 的治疗与对照组相比，在2周的治疗期内，以1 mg/kg的剂量抑制了后爪体积增加50%，而以3或10 mg/kg的剂量则抑制超过95%。由于在治疗第0天，即动物出现明显病征时对爪体积的基线测量，对于那些在肿胀明显好转的动物，抑制率可能超过100%[1]。Baricitinib (0.7 mg/天)处理的小鼠，通过H&E染色评估，表现出明显减少的炎症，CD8浸润减少，以及MHC I类和II类表达降低，与对照组相比有显著差异。在与对照组相比，Baricitinib处理的小鼠中，对于鼠和人类斑秃(AA)疾病中关键的效应细胞CD8+NKG2D+细胞大幅减少[2]。
激酶实验	Enzyme assays are performed using a homogeneous time-resolved fluorescence assay with recombinant epitope tagged kinase domains (JAK1, 837-1142; JAK2, 828-1132; JAK3, 718-1124; Tyk2, 873-1187) or full-length enzyme (cMET and Chk2) and peptide substrate. Each enzyme reaction is performed with or without test compound (11-point dilution), JAK, cMET, or Chk2 enzyme, 500 nM (100 nM for Chk2) peptide, ATP (at the Km specific for each kinase or 1 mM), and 2.0% DMSO in assay buffer. The calculated IC50 value is the compound concentration required for inhibition of 50% of the fluorescent signal. Additional kinase assays are performed at Cerep using standard conditions at 200 nM. Enzymes tested included: Abl, Akt1, AurA, AurB, CDC2, CDK2, CDK4, CHK2, c-kit, EGFR, EphB4, ERK1, ERK2, FLT-1, HER2, IGF1R, IKKα, IKKβ, JNK1, Lck, MEK1, p38α, p70S6K, PKA, PKCα, Src, and ZAP70[1].
细胞实验	Baricitinib(INCB 028050) is dissolved in stock solutions, and then diluted with appropriate media before use[1]. Human PBMCs are isolated by leukapheresis followed by Ficoll-Hypaque centrifugation. For the determination of IL-6-induced MCP-1 production, PBMCs are plated at 3.3×105 cells per well in RPMI 1640+10% FCS in the presence or absence of various concentrations of INCB028050 (1 nM, 10 nM, 100 nM, 1 μM, and 10 μM). Following preincubation with compound for 10 min at room temperature, cells are stimulated by adding 10 ng/mL human recombinant IL-6 to each well. Cells are incubated for 48 h at 37°C, 5% CO2. Supernatants are harvested and analyzed by ELISA for levels of human MCP-1. The ability of INCB028050 to inhibit IL-6-induced secretion of MCP-1 is reported as the concentration required for 50% inhibition (IC50). Proliferation of Ba/F3-TEL-JAK3 cells is performed over 3 d using Cell-Titer Glo[1].
别名	磷酸巴瑞克替尼, LY-3009104 phosphate, INCB-028050 phosphate, Baricitinib Phosphate

化学信息

分子量	469.41
分子式	C₁₆H₂₀N₇O₆PS
CAS No.	1187595-84-1
Smiles	OP(O)(O)=O.CCS(=O)(=O)N1CC(CC#N)(C1)n1cc(cn1)-c1ncnc2[nH]ccc12
密度	no data available

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

实际储存温度请以COA为准

溶解度信息

DMSO: 50 mg/mL (106.52 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.26 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1303 mL	10.6517 mL	21.3033 mL	106.5167 mL
5 mM	0.4261 mL	2.1303 mL	4.2607 mL	21.3033 mL
10 mM	0.2130 mL	1.0652 mL	2.1303 mL	10.6517 mL
20 mM	0.1065 mL	0.5326 mL	1.0652 mL	5.3258 mL
50 mM	0.0426 mL	0.2130 mL	0.4261 mL	2.1303 mL
100 mM	0.0213 mL	0.1065 mL	0.2130 mL	1.0652 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

Baricitinib phosphate

Baricitinib phosphate

产品介绍

计算器

体内实验配液计算器

剂量转换

引用文献

关键词

Baricitinib phosphate

Baricitinib phosphate