Baricitinib (Synonyms: 巴瑞替尼; LY3009104; INCB028050)
目录号: PL04412 纯度: ≥99%

Baricitinib (LY3009104; INCB028050) 是选择性,可口服的 JAK1 和 JAK2 抑制剂,IC50 分别为5.9 nM 和 5.7 nM。

CAS No. :1187594-09-7
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中文名称
Baricitinib
中文别名
巴瑞克替尼;巴瑞替尼(BARICITINIB);1-(乙基磺酰基)-3-[4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基]-3-氮杂环丁烷乙腈;Baricitinib (LY3009104, INCB028050) 抑制剂;巴里西替尼;巴瑞克替尼(Baricitinib);巴瑞替尼;磺酰基)-3-[4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基]-3-氮
英文名称
Baricitinib
英文别名
Baricitinib (INCB28050, LY3009104);1-(Ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile;Baricitinib;2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile;Baricitinib (LY3009104, INCB028050);JAK inhibitor;{1-(ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile;2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile;3-Azetidineacetonitrile,1-(ethylsulfonyl)-3-(4-(7H-pyrrolo(2,3-d)pyrimidin-4-yl)-1H-pyrazol-1-yl);INCB 028050;INCB-028050;LY 3009104;LY-3009104;INCB028050;LY3009104;ISP4442I3Y;INCB 28050;C16H17N7O2S;olumiant;3-AZETIDINEACETONITRILE, 1-(ETHYLSULFONYL)-3-[4-(7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL]-;Bar;Baricitinib [U
Cas No.
1187594-09-7
分子式
C16H17N7O2S
分子量
371.42
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Baricitinib (LY3009104; INCB028050) 是选择性,可口服的 JAK1 和 JAK2 抑制剂,IC50 分别为5.9 nM 和 5.7 nM。
生物活性
Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC 50 s of 5.9 nM and 5.7 nM, respectively.
性状
Solid
IC50 & Target[1][2]
JAK2 5.7 nM (IC50) JAK1 5.9 nM (IC50
体外研究(In Vitro)
In cell-based assays, Baricitinib (INCB028050) proves to be a potent inhibitor of JAK signaling and function. In PBMCs, Baricitinib inhibits IL-6-stimulated phosphorylation of the canonical substrate STAT3 (pSTAT3) and subsequent production of the chemokine MCP-1 with IC50 values of 44 nM and 40 nM, respectively. In isolated naive T-cells, INCB028050 also inhibits pSTAT3 stimulated by IL-23 (IC50=20 nM). Importantly, this inhibition prevented the production of two pathogenic cytokines (IL-17 and IL-22) produced by Th17 cells-a subtype of helper T cells with demonstrable inflammatory and pathogenic properties-with an IC50 value of 50 nM. In stark contrast, the structurally similar but ineffective JAK1/2 inhibitors INCB027753 and INCB029843 has no significant effect in any of these assays systems when tested at concentrations up to 10 μM.
体内研究(In Vivo)
Baricitinib (INCB028050) treatment, compares with vehicle, inhibits the increase in hind paw volumes during the 2 wk of treatment by 50% at a dose of 1 mg/kg and >95% at doses of 3 or 10 mg/kg. Because baseline paw volume measurements are taken on treatment day 0-in animals with significant signs of disease-it is possible to have >100% inhibition in animals showing marked improvement in swelling. Baricitinib (0.7 mg/day) treated mice exhibits substantially reduced inflammation as assessed by H&E staining, reduced CD8 infiltration, and reduced MHC class I and class II expression when compared with vehicle-control treated mice. CD8NKG2D cells, critical effectors of disease in murine and human alopecia areata (AA), are greatly diminished in Baricitinib treated mice compare with vehicle control treated mice. has n
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Fridman JS, et al. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J Immunol. 2010 May 1;184(9):5298-307.
[2]. Jabbari A, et al. Reversal of Alopecia Areata Following Treatment With the JAK1/2 Inhibitor Baricitinib. EBioMedicine. 2015 Feb 26;2(4):351-5.
溶解度数据
In Vitro: DMSO : 25 mg/mL (67.31 mM; Need ultrasonic and warming)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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