Baricitinib (INCB028050)

For research use only. Not for use in humans.

目录号:S2851 别名: LY3009104 中文名称:巴瑞克替尼

Baricitinib (INCB028050) Chemical Structure

CAS No. 1187594-09-7

Baricitinib (LY3009104, INCB028050)是一种选择性JAK1JAK2抑制剂,无细胞试验中IC50分别为5.9 nM和5.7 nM,比作用于JAK3和Tyk2选择性高70和10倍左右,对c-Met和Chk2没有抑制作用。Baricitinib被发现可以减少或干扰病毒进入目标细胞,并用于COVID-19的治疗研究中。Phase 3

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2211.3 现货
RMB 2224.19 现货
RMB 3029.99 现货
RMB 8763.3 现货
RMB 20229.3 现货
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客户使用Selleck生产的Baricitinib (INCB028050)发表文献17篇:

客户使用该产品的4个实验数据:

  • bDNA analysis showing that the JAK1/2 inhibitors CYT387, AZD1480 and Baricitinib positively regulate UCP1 expression in PSC-WA. Values are mean ± s.d. of n = three biological replicates and differences from DMSO are significant for * P < 0.005. P values were calculated using the two-tailed paired Student's t-test.

    Nat Cell Biol,2014, 17(1):57-67. Baricitinib (INCB028050) purchased from Selleck.

  • (A-C) Anti-proliferative activity of NDI-031301 (A), tofacitinib (B) or baricitinib (C) on transformed Ba/F3 cells. Ba/F3 cells transformed by TEL-ABL, TEL-JAK1, TEL-JAK2, TEL-JAK3, or TEL-TYK2 were cultured with graded concentrations of the indicated inhibitor for 72 h. Cell viability values are mean SD percentages of the untreated control value in triplicate experiments.

    Br J Haematol, 2017, 177(2):271-282. Baricitinib (INCB028050) purchased from Selleck.

  • HT‐29/B6‐GR/MR cells were stimulated with or without DBA and with or without IL‐13 in the presence or absence of baricitinib or AS1517499 for 96 h, then rested FCS and IL‐13 free for 3 h and treated again with IL‐13 for 30 min. Then, total cellular protein was extracted, fractionated by SDS‐Page, and immuno‐probed for phospho‐specific ERK1/2, JNK, p38, or STAT6 expression. Human β‐actin served as loading control.

    J Physiol, 2015, 593(24):5269-82. Baricitinib (INCB028050) purchased from Selleck.

  • JAK inhibitors work on “type 17” cytokine production in-vitro in Spondyloarthritis on established peripheral Th17 cells and on synovial fluid CD4+ T cells. (a) Reduction of IL-17A secretion by JAK inhibitors (Tofa, JAK3 > JAK1/2; Ruxo, JAK2 > JAK1; Bari, JAK1/2 > TYK2; CEP, JAK2) in AS CD4+ T cells (n = 6), primed under Th17-promoting conditions for 6 days, upon restimulation with anti-CD2/3/28 beads for 24 hours measured by ELISA. (b) Effects of JAK inhibitors on IL-17A secretion (ELISA) from synovial CD4+ T cells of SPA patients cultured for 3 days (n = 4, Bari n = 3). Statistical analysis: mean ± SEM, repeated measures 1-way ANOVA followed by Dunnett’s method for multiple comparisons. Bari:Baricitinib.

    Sci Rep, 2018, 8(1):15645. Baricitinib (INCB028050) purchased from Selleck.

产品安全说明书

JAK抑制剂选择性比较

生物活性

产品描述 Baricitinib (LY3009104, INCB028050)是一种选择性JAK1JAK2抑制剂,无细胞试验中IC50分别为5.9 nM和5.7 nM,比作用于JAK3和Tyk2选择性高70和10倍左右,对c-Met和Chk2没有抑制作用。Baricitinib被发现可以减少或干扰病毒进入目标细胞,并用于COVID-19的治疗研究中。Phase 3
靶点
JAK2 [1]
(Cell-free assay)
JAK1 [1]
(Cell-free assay)
TYK2 [1]
(Cell-free assay)
JAK3 [1]
(Cell-free assay)
5.7 nM 5.9 nM 53 nM >400 nM
体外研究

在外周血单核细胞中Baricitinib抑制IL-6刺激的典型底物STAT3 (pSTAT3) 的磷酸化以及随后趋化因子MCP-1的产生,IC50值分别为44 nM和40 nM。在独立的幼稚型T 细胞中Baricitinib也可以抑制IL-23刺激的STAT3的磷酸化,IC50为20 nM [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human CD34+ cells MXrGeY5kfGmxbjDhd5NigQ>? M2T1R|Q2KG2rboO= NGXjNYtKdmirYnn0bY9vKG:oIFrBT|IhcG:vb3TpcYVzKGmwIHj1cYFvKEOGM{SrJINmdGy|IIPwbYtm\CCrboTvJIh2dWGwIIfoc4xmKGKub3;kJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gSXBQNWmwZIXj[YQhW1SDVD21JJBpd3OyaH;yfYxifGmxbjDwdoVqdmO3YnH0[YQh\m:{IES1JI1qdnNiZn;scI94\WRiYomgSXBQKGGmZHn0bY9vKG2nYYP1doVlKGGodHXyJFE2KG2rboOgZpkhTkGFUzDhcoFtgXOrczygTWM2OD1yLkC4O|jPxE1? NWjWZWF2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0NVc2OzNpPkK0OFE4PTN|PD;hQi=>
human UT7 cells NYjmWHZnTnWwY4Tpc44h[XO|YYm= M2q1fGlvcGmkaYTpc44hd2ZiSlHLNkBqdiCqdX3hckBWXDdiY3XscJMh[XO|ZYPz[YQh[XNic4XwdJJme3Orb36gc4YhTVCRLYP0bY12dGG2ZXSgV3RCXDVicHjvd5Bpd3K7bHH0bY9vKGK7IFHsdIhiW2O{ZXXuJIF{e2G7 MofEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|N{K2OVMoRjJ4M{eyOlU{RC:jPh?=
human TF1 cells NU\6eol6TnWwY4Tpc44h[XO|YYm= MlnrTY5pcWKrdHnvckBw\iCMQVuxJIlvKGi3bXHuJHRHOSClZXzsd{Bie3Onc4Pl[EBieyC|dYDwdoV{e2mxbjDv[kBKVDZvc4TpcZVt[XSnZDDTWGFVOyCyaH;zdIhwenmuYYTpc44h[nliQXzwbIFU[3KnZX6gZZN{[Xl? M1vDVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{eyOlU{Lz5{NkO3NlY2OzxxYU6=
CD34+ MmntSpVv[3Srb36gZZN{[Xl? MlPSOFUhdWmwcx?= MnzoTY5pcWKrdHnvckBw\iCMQVuyJIhwdW:maX3ldkBqdiCqdX3hckBETDN2KzDj[YxteyC|cHnr[YQhcW62bzDoeY1idiC5aH;s[UBjdG:xZDDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFXQU{1qdmS3Y3XkJHNVSVRvNTDwbI9{eGixconsZZRqd25icILlbY5kfWKjdHXkJIZweiB2NTDtbY5{KG[xbHzve4VlKGK7IFXQU{Bi\GSrdHnvckBu\WG|dYLl[EBi\nSncjCxOUBucW6|IHL5JGZCS1NiYX7hcJl{cXNuIFnDOVAhRSByLkC4O|gh|ryPLh?= NHXDfnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NESxO|U{Oyd-MkS0NVc2OzN:L3G+
TF1 NF;xZoFHfW6ldHnvckBie3OjeR?= MV;Jcohq[mm2aX;uJI9nKEqDS{GgbY4hcHWvYX6gWGYyKGOnbHzzJIF{e2W|c3XkJIF{KHO3cIDy[ZN{cW:wIH;mJGlNPi2|dHnteYxifGWmIGPURXQ{KHCqb4PwbI9zgWyjdHnvckBjgSCDbIDoZXNkemWnbjDhd5NigSxiSV7IJF0hOC5yMUeg{txONg>? NIDOd4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO3NlY2Oyd-Mk[zO|I3PTN:L3G+
UT7 MYrGeY5kfGmxbjDhd5NigQ>? M37OemlvcGmkaYTpc44hd2ZiSlHLNkBqdiCqdX3hckBWXDdiY3XscJMh[XO|ZYPz[YQh[XNic4XwdJJme3Orb36gc4YhTVCRLYP0bY12dGG2ZXSgV3RCXDVicHjvd5Bpd3K7bHH0bY9vKGK7IFHsdIhiW2O{ZXXuJIF{e2G7LDDJUmghRSByLkOxJO69VS5? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN5Mk[1N{c,OjZ|N{K2OVM9N2F-
HeLa M3HyUWZ2dmO2aX;uJIF{e2G7 NEDLOlQ2KHWP NWDqXnlYOiCqcoO= MXrJcohq[mm2aX;uJI9nKEmITnfhcY1iNWmwZIXj[YQhUkGNMjDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iSHXMZUBk\WyuczDheEA2KHWPIHnuZ5Vj[XSnZDDmc5IhOiCqcoOgZpkhX2W|dHXyckBjdG:2IH3leIhw\A>? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF|N{O1PUc,OjdzM{ezOVk9N2F-
A673 NILPNVZyUFSVIHHzd4F6 MUfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? NX32UVVjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH NE\Mbm9yUFSVIHHzd4F6 NG\pU4pyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1UUCClZXzsdy=> NWi0XotpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 MVzxTHRUKGG|c3H5 NX\kPXdXeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> Moe0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 MUTxTHRUKGG|c3H5 M1TZUJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaESxJINmdGy| MlLNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 M{XIeJFJXFNiYYPzZZk> MWPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? MnHIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
phSTAT1 / phSTAT3 ; 

PubMed: 28369741     


Effect of Janus kinase (JAK) inhibition on phosphorylated signal transducer and activator of transcription (STAT) phosphorylation in RA neutrophils. Freshly isolated (0 h) RA neutrophils exhibited elevated levels of STAT-1 and STAT-3, which decreased during 60 min incubation in untreated conditions. Addition of baricitinib and tofacitinib (200 ng/ml) at 0 h induced a loss of phosphorylated STAT-1 and STAT-3 compared to untreated cells at 30 and 60 min.

28369741
体内研究 Baricitinib在全血中抑制IL-6刺激的STAT3磷酸化,IC50为128 nM。 Baricitinib (10 mg/kg口服)预期能够在大鼠中抑制JAK1/2 信号 (抑制率≥50%)达8小时。Baricitinib (10mg/mL,口服)可以抑制佐剂性关节炎大鼠模型的疾病得分并且具有剂量依赖特性。与对照组相比,1mg/kg Baricitinib处理两周可以对雌鹿爪子体积增长抑制50%,3 mg/kg 或10 mg/kg剂量可以抑制95%以上。与对照组相比,1mg/kg Baricitinib处理可以对佐剂性关节炎大鼠模型免疫浸润,水肿,和关节周围组织外观的综合得分抑制27%,3mg/kg可以抑制64%,10 mg/kg可以抑制82%。1, 3和10 mg/kg Baricitinib分别使佐剂性关节炎大鼠模型骨吸收减少15%, 61%和67%。Baricitinib (10mg/kg,每天一次连续2周,口服)可以使佐剂性关节炎大鼠模型踝关节和跗骨的正常结构和外观得到影像学上的改善。Baricitinib可以降低达拉亚动物外周血中STAT3的磷酸化水平,并且具有剂量和时间依赖的特性。Baricitinib (10 mg/mL, 口服)可以使小鼠胶原蛋白诱导的关节炎(CIA)模型的关节损伤综合得分提高47%。在胶原抗体诱导的关节炎(CAIA)小鼠模型中Baricitinib (10 mg/kg) 可以减少血管翳 (74%)和骨损伤(78%),改善软骨损伤 (43%)和炎症信号 (33%), 使疾病综合得分提高53%。在CIA和CAIA模型中,Baricitinib (10 mg/kg)可以对迟发型超敏反应抑制48%[1]。 Baricitinib对于活动性类风湿关节炎病人是有效的,而疾病修饰药物和生物制剂大多很难有效[2]。 Baricitinib优先抑制JAK1 和 JAK2, 选择性高于Tyk2 10倍,高于JAK3 100倍。观察到的GLPG-0634对于ACR20的效果至少和tofacitinib一样而且优于Baricitinib, 因为Baricitinib 仅在一项二期临床实验中可以适度地影响ACR20值[3]。 Baricitinib具有剂量限制的副作用,会诱发贫血病,这是由于对JAK2的影响造成的,但是无论如何它的药效非常明确[4]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验:[1]
- 合并
  • Animal Models: 胶原蛋白诱导的关节炎(CIA)小鼠模型
  • Dosages: 10 mg/mL
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 74 mg/mL (199.23 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 371.42
化学式

C16H17N7O2S

CAS号 1187594-09-7
储存条件 粉状
溶于溶剂
别名 LY3009104

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04208464 Not yet recruiting Drug: Baricitinib Idiopathic Inflammatory Myopathies University of Manchester|Eli Lilly and Company|Manchester Clinical Trials Unit|Karolinska Institutet July 1 2020 Phase 2
NCT04358614 Completed Drug: Baricitinib 4 MG Oral Tablet COVID|Pneumonia Fabrizio Cantini|Hospital of Prato March 16 2020 Phase 2|Phase 3
NCT04088396 Recruiting Drug: Baricitinib|Drug: Placebo Systemic Juvenile Idiopathic Arthritis Eli Lilly and Company February 12 2020 Phase 3
NCT03952559 Recruiting Drug: Baricitinib|Drug: Placebo|Drug: Topical corticosteroid Atopic Dermatitis Eli Lilly and Company|Incyte Corporation May 24 2019 Phase 3
NCT03773978 Recruiting Drug: Baricitinib|Drug: Placebo Juvenile Idiopathic Arthritis Eli Lilly and Company December 17 2018 Phase 3

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    Do you know if S2851 will dissolve directly into 0.5% methylcellulose (vehicle for oral gavage treatments) or is acid required to dissolve it?

  • 回答:

    S2851 dissolve directly into 0.5% methylcellulose, and this is cited from the reference. We also test that dissolve S2851 into 30% PEG400/0.5% Tween80/5% propylene glycol. The solubility is about 30 mg/mL.

JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID